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1

Luna, Isadora Silva, Rayssa Marques Duarte da Cruz, Ryldene Marques Duarte da Cruz, Rodrigo Santos Aquino de Araújo, and Francisco Jaime Bezerra Mendonça-Junior. "1,4-Dithiane-2,5-diol: A Versatile Synthon for the Synthesis of Sulfur-containing Heterocycles." Current Organic Synthesis 15, no. 8 (December 17, 2018): 1026–42. http://dx.doi.org/10.2174/1570179415666180821154551.

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Background: 1,4-Dithiane-2,5-diol (1,4-DTD) is the stable dimer of α-mercapto acetaldehyde. This commercially available ambidentade compound is characterized as having in its chemical structure one group that acts as an electrophile and another that acts as a nucleophile, this permits its use as versatile and efficient synthon in synthetic heterocycle procedures. Objective: The aim of this review is to present synthetic applications of 1,4-DTD in heterocyclic chemistry and their applicability to the synthesis of bioactive compounds. Conclusion: Gewald reactions to obtain C-4 and C-5 unsubstituted 2-amino-thiophene derivatives; sulfa- Michael/Henry and sulfa-Michael/aldol sequences to obtain polysubstituted tetrahydrothiophenes, and other heterocyclic reactions that allow synthesizing several functionalized sulfur-containing heterocycles such as thiazolidines, oxathiazinoles and thiazoles are presented and discussed. The use of such heterocyclics in subsequent reactions allows obtaining various bioactive compounds including the antiretroviral lamivudine which is one of the examples presented in this review.
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2

Yadav, Shailendra, Sushma Singh, and Chitrasen Gupta. "A CONCISE OVERVIEW ON HETEROCYCLIC COMPOUNDS EXHIBITING PESTICIDAL ACTIVITIES." International Journal of Advanced Research 9, no. 08 (August 31, 2021): 989–1004. http://dx.doi.org/10.21474/ijar01/13352.

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Heterocyclic compounds are numerous and diverse group of organic compounds. Heterocycles are abundantly found in nature and express various physiological properties. Heterocycles are intricately linked to all aspects of life. There are many heterocyclic compounds currently known, and the number is constantly rising owing to extensive synthetic development and their applications. Heterocyclic compounds are used significantly in a number of areas, including biochemistry and medicinal chemistry, and some others. They are predominantly synthesized in agrochemical and pharmaceutical industries due to their potential biological activities. This review article focuses on recently synthesized heterocyclic compounds and their different pesticidal activities such as antifungal, antibacterial, antiviral, nematocidal, insecticidal, acaricidal, and herbicidal.
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3

Romero-Hernández, Laura L., Ana Isabel Ahuja-Casarín, Penélope Merino-Montiel, Sara Montiel-Smith, José Luis Vega-Báez, and Jesús Sandoval-Ramírez. "Syntheses and medicinal chemistry of spiro heterocyclic steroids." Beilstein Journal of Organic Chemistry 20 (July 24, 2024): 1713–45. http://dx.doi.org/10.3762/bjoc.20.152.

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There is compelling evidence that incorporating a heterocyclic moiety into a steroid can alter its pharmacological and pharmacokinetic properties, driving intense interest in the synthesis of such hybrids among research groups. In this review, we present an overview of recent synthetic methodologies, spanning the period from 2000 to 2023, for the preparation of spiro heterocyclic steroids. The compounds surveyed encompass four-, five-, six-, and seven-membered heterocycles appended to various positions of steroidal backbones, with spirocycles containing oxygen, nitrogen, and sulfur atoms being predominant. The outlined synthetic procedures emphasize the pivotal steps for constructing the heterocycles, often accompanied by a detailed account of the overall synthesis pathway. The review encompasses innovative compounds, including bis-steroids linked by a spiro heterocycle and steroids conjugated to heterocyclic moieties containing three or more (hetero)cycles. Moreover, many compounds are accompanied by data on their biological activities, such as antiproliferative, antimalarial, antimicrobial, antifungal, steroid antagonist, and enzyme inhibition, among others, aimed at furnishing pertinent insights for the future design of more potent and selective drugs.
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4

Bhattacharya, Somenath, Soumallya Chakraborty, Rohan Pal, Sourav Saha, Bhaskar Ghosh, Chiranjit Mandal, Dr Amitava Roy, and Dr Arin Bhattacharjee. "A Comprehensive Review on Pyrazole and It’s Pharmacological Properties." International Journal for Research in Applied Science and Engineering Technology 10, no. 9 (September 30, 2022): 1769–74. http://dx.doi.org/10.22214/ijraset.2022.46924.

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Abstract: Heterocyclic chemistry is very important aspects in organic chemistry. Heterocyclic system consists of one or more heteroatoms like nitrogen, oxygen, sulphur, etc with hydrogen atoms. The system can be classified as saturated as well as non saturated system or hydrocarbons. Another classification of this ring system is divided in some categories like three-membered, four-membered, five-membered, six-memebered, seven-membered, fused heterocyclics etc. Some compounds under this cklassification are acidic or basic in nature. Examples of heterocyclic compounds are Pyrole, Furan, Thiophene, Pyridine, Quinoline, Isoquinoline, Indole, Purine, Pyrazole, etc. Pyrazole is very important under this heterocyclic ring sysyem. Pyrazole is five membered heterocyclics. Pyrazole is basic and unsaturated in nature due to presence of double bonds in their ring structure. When two nitrogen atoms are associated with five menbered heterocyclic ring in 1,2 positions called as Pyrazole structure. It is also known as 1,2-diazole. It is present in many drugs as well as organic compounds and Pharmaceutical compounds. The review study shown that the structure, physical and chemical properties, nomenclature, synthetic approaches, biological activities of Pyrazole heterocyclic ring structure
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5

K. Slman, Dhuha, Hind A. Satar, Zahraa A. Ketan, and Asmaa A. Jawad. "Heterocyclic Compounds: A Study of its Biological Activity." Al-Nahrain Journal of Science 27, no. 5 (December 1, 2024): 19–24. https://doi.org/10.22401/anjs.27.5.03.

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Heterocyclic compounds have gained a lot of attention because of their numerous significant medical and biological uses. Research interest on heterocyclic compounds is rapidly increasing due to the extensive synthetic study and functional utility. Heterocycles also play a role in different fields, inclusive of medicinal chemistry, biochemistry, and others. Pharmaceuticals, agrochemicals, and veterinary items are the main applications of heterocyclic compounds. In our review, we cover the majority of bio-active heterocycles that have recently been synthesized and introduced a new phase of possible antifungal, anti-inflammatory, anti-bacterial, antiviral, antioxidant, and other medical applications.
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6

Palaniappan, Saravana Priya. "Pharmacological Role of Heterocyclic Compounds in the Treatment of Alzheimer’s Disease: A Review." Journal of Phytopharmacology 11, no. 4 (August 15, 2022): 289–94. http://dx.doi.org/10.31254/phyto.2022.11412.

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Alzheimer’s disease (AD) is a multifactorial neurological disease that mainly affects the old age people. Neuropathologically, AD is characterized by low level of acetylcholine, loss of synapses and neurons in certain brain regions, accumulation of extracellular amyloid beta peptide (Aβ) and phosphorylation of intracellular tau protein. Patients with AD are characterized by various symptoms such as memory deficits, depression, cognitive dysfunction and difficult to perform daily activities. Currently available drugs for the treatment of AD are used to treat symptomatic relief at an early stage, however the prolonged usage of the drugs may cause adverse side effects. To overcome this, development of drugs produced from natural products is considered as one of the promising alternatives for the treatment of AD. Among that heterocyclic compound play a major role in the development of therapeutic drugs against various disorders. An organic compound which is cyclic or non-cyclic consists of one or more atoms in their ring structure are known as heterocyclic compounds. These heterocyclic compounds occur both in natural and synthetic form and play a major role in the metabolism of all living cells. Most of the organic compounds used as drugs have a heterocyclic core in their skeleton. Nitrogenous bases such as purines and pyrimidines present in DNA, chlorophyll, vitamins contain heterocycle in their structure. Other compounds containing heterocycles are proline, morphine, furan, vinblastine, cephalosporin, penicillin etc. This review summarizes the nomenclature, classification, and the role of heterocyclic compounds in the treatment of Alzheimer's disease.
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7

Mr., Mayur Ashok Patkari, Roshan M. Chaudhari Mr., Hitendra S. Chaudhari Mr., and S. P. Pawar Dr. "A Review on Heterocyclic Compound Containing Anticancer Agent, As A Medicinal Chemistry Perspective." Journal of Advances in Clinical Pharmacology 2, no. 1 (December 7, 2023): 27–38. https://doi.org/10.5281/zenodo.10279377.

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<i>One of the main causes of death in the globe is cancer. Cancer is caused by gene and protein regulation errors in cells. Despite their side effects, surgery, radiation therapy, and the use of anticancer drugs constitute the contemporary cancer therapy. Heterocyclic chemistry is the general field of study. The article's goal is to cover the most current developments in heterocyclic nitrogen compounds as potential cancer chemotherapeutic agents. Heterocyclics make up more than 80% of new medications, and those that contain nitrogen have better pharmacological effects than those that do not. Compounds containing nitrogen, the foundation of drug development, are an important and valuable class of chemicals that are essential to living cells' metabolism. Medications that are physiologically active comprise more than 85% heterocycles, or at least one heteroatom. We have listed the pharmacological characteristics of FDA-approved heterocyclic medications containing nitrogen atoms in this study. Additionally, we have reported nitrogen-containing heterocycles that are used to treat various cancer types while concurrently covering the cellular targets and biochemical mechanisms of action, such as pyrimidine, quinolone, carbazole, pyridine, imidazole, benzimidazole, triazole, ß-lactam, indole, pyrazole, quinazoline, quinoxaline, isatin, pyrrolo-benzodiazepines, and pyrido[2,3-d]pyrimidines.</i>
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8

Shaikh, Ansar R., Mazahar Farooqui, R. H. Satpute, and Syed Abed. "Overview on Nitrogen containing compounds and their assessment based on ‘International Regulatory Standards’." Journal of Drug Delivery and Therapeutics 8, no. 6-s (December 21, 2018): 424–28. http://dx.doi.org/10.22270/jddt.v8i6-s.2156.

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Heterocyclic compounds have a role in most fields of sciences such as medicinal chemistry, biochemistry also another area of sciences. More than 90% of new drugscontain heterocycles and the interface between chemistry and biology, at which so much new scientific insight, discovery and application is taking place is crossed by heterocyclic compounds. Compounds derived from heterocyclic rings in pharmacy, medicine, agriculture, plastic, polymer and other fields.Most active heterocycles that have shown considerable biological actions as antifungal, anti-inflammatory, antibacterial, anticonvulsant, antiallergic, herbicidal, anticancer activity. There is always a strong need for new and efficient processes in synthesizing of new Heterocycles.Alum have been used as a novel catalyst in the synthesis of Schiff’s bases. Synthesized Schiff’s bases are free from use of ICH class 1 and Class 2 solvents and also free from structural alerts genotoxic impurities. This review highlights on various aspects of heterocyclic compounds with its biological activity &amp; regulatory assessment based on the ‘International Regulatory Standards’.&#x0D; Keywords: Heterocycles. Nitrogen containing compounds Biological activity, History, Regulatory assessment, International Regulatory Standards
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9

Adak, Laksmikanta, and Tubai Ghosh. "Recent Progress in Iron-Catalyzed Reactions Towards the Synthesis of Bioactive Five- and Six-Membered Heterocycles." Current Organic Chemistry 24, no. 22 (December 18, 2020): 2634–64. http://dx.doi.org/10.2174/1385272824999200714102103.

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Heterocyclic compounds are the largely diverse organic molecules and find prevalent applications in the fine chemical industry, medicinal chemistry and agricultural science. They are also among the most commonly bearing frameworks in numerous drugs and pharmaceutical substances. Therefore, the development of convenient, efficient and environmentally benign methods to produce various types of heterocyclic compounds is an attractive area of research. For the synthesis and functionalization of heterocycles, enormous achievements have been attributed over the past decades. Recently, ironcatalyzed reactions have accomplished a noteworthy development in the synthesis of heterocycles. This review highlights some remarkable achievements in the iron-catalyzed synthesis of heterocyclic compounds published in the last five years.
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10

Olšovská, Jana, Karel Štěrba, Martin Slabý, and Tomáš Vrzal. "Novel method for determination of heterocyclic compounds and their impact in brewing technology." KVASNY PRUMYSL 67, no. 2 (April 15, 2021): 417–27. http://dx.doi.org/10.18832/kp2021.67.417.

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A new simultaneous method for determination of 16 heterocyclic compounds using SPE sample preparation and GC-MS determination was developed regarding increasing interest of the role of sensory active compounds in beer. LiChrolut® EN SPE columns proved to be optimal for both, a mixture of analytes with a different polarity and such complicated matrix as beer. Recoveries of individual analytes are about 100% except for three compounds (2-methylpyridine about 30%, maltol and furaneol about 50%); repeatability, uncertainty and LOQ are satisfactory for the method application. The method was used for monitoring of heterocyclic compounds formation during roasting, mashing, hop boiling and fermentation. To summarize, during roasting of malt, the concentration of oxygen heterocycle compounds (OHC) increases more rapidly in comparison with nitrogen heterocycles compounds (NHC) till a critical point where OHC starts to decrease and NHC starts to be formed sharper (with the exception of 2-acetylpyrrole which is similar to OHC). Finally, the total concentration of NHC during fermentation rapidly decreases whilst the OHC concentration is influenced by many factors, e.g., fermentation conditions and yeast strain.
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11

Negi, Beena, and Aarshiya Kwatra. "A Review of Recent Progress on the Anticancer Activity of Heterocyclic Compounds." SynOpen 08, no. 03 (August 2024): 185–210. http://dx.doi.org/10.1055/s-0040-1720125.

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AbstractCancer is one of the most daunting illnesses in the world as compared to many other human diseases. This review article aims to summarize the literature that is already published based on heterocyclic anticancer compounds. Under this broad topic we try to shed a light on anticancer potentiality of oxygen-, sulfur-, and nitrogen-containing heterocyclic compounds, such as quinolines, pyrroles, pyrimidines, pyridines, indoles, also sulfonamides linked heterocycles, benzimidazoles and oxadiazoles.1 Introduction1.1 Drugs in Use for Cancer Treatment1.2 Recently Discovered Anticancer Drugs2 Various Classes of Compounds as Anticancer Agents2.1 Quinoline Derivatives as Anticancer Agents2.2 Benzimidazoles as Anticancer Agents2.3 Indole: A Privileged Scaffold for the Design of Anticancer Agents2.4 Pyrimidine Derivatives as Anticancer Agents2.5 Pyridine Derivatives as Anticancer Agents2.6 Pyrrole Derivatives as Anticancer Agents2.7 Sulfonamides linked with heterocycles as Anticancer Agents2.8 Oxadiazole and Its Derivatives as Anticancer Compounds2.9 Benzothiazole-Triazole Hybrids as Anticancer Compounds3 Conclusion
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12

Murarka, Sandip, and Andrey Antonchick. "Metal-Catalyzed Oxidative Coupling of Ketones and Ketone Enolates." Synthesis 50, no. 11 (May 3, 2018): 2150–62. http://dx.doi.org/10.1055/s-0037-1609715.

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Recent years have witnessed a significant advancement in the field of radical oxidative coupling of ketones towards the synthesis of highly useful synthetic building blocks, such as 1,4-dicarbonyl compounds, and biologically important heterocyclic and carbocyclic compounds. Besides oxidative homo- and cross-coupling of enolates, other powerful methods involving direct C(sp3)–H functionalizations of ketones­ have emerged towards the synthesis of 1,4-dicarbonyl compounds. Moreover, direct α-C–H functionalization of ketones has also allowed an efficient access to carbocycles and heterocycles. This review summarizes all these developments made since 2008 in the field of metal-catalyzed/promoted radical-mediated functionalization of ketones at the α-position.1 Introduction2 Synthesis of 1,4-Dicarbonyl Compounds3 Synthesis of Heterocyclic Scaffolds4 Synthesis of Carbocyclic Scaffolds5 Conclusion
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13

Huang, Pengfei, Pan Wang, Shengchun Wang, Shan Tang, and Aiwen Lei. "Electrochemical oxidative [4 + 2] annulation of tertiary anilines and alkenes for the synthesis of tetrahydroquinolines." Green Chemistry 20, no. 21 (2018): 4870–74. http://dx.doi.org/10.1039/c8gc02463d.

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14

Shekarkhand, Marzieh, Karim Zare, Majid Monajjemi, Elham Tazikeh-Lemeski, and Masoumeh Sayadian. "Computational study of heterocyclic anticancer compounds through nbo method." Nexo Revista Científica 35, no. 01 (April 6, 2022): 367–81. http://dx.doi.org/10.5377/nexo.v35i01.13982.

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In the present study NBO method contain the HOMO and the LUMO energies are calculated for 10 different heterocycles anticancer drug using B3LYP/6-31G(d,p). Frontier molecular orbitals (HOMO and LUMO) and Molecular Electrostatic Potential map of the compound was produced by using the π stacking of structures and anticancer activity of molecules. The NBO analysis was suggested that the molecular system contains π- π interaction, strong conjugative interactions and the molecule become more polarized owing to the movement of π-electron cloud from donor to acceptor. NBO, HOMO and LUMO energies, were investigated and Anticancer activity of Aromatic Heterocyclic compounds was investigated by NBO study and result was compared with our previous study about NICS and S-NICS of these 10 anticancer drug. the HOMO/LUMO gap of the heterocycle anticancer drug is significantly different from each other. The NBO method is used in both symmetric and asymmetric molecules and provides accurate information on the aromatics of the compound, especially the heterocyclic rings. It also provides accurate information in protected areas. Molecule 8 has the highest amount of HOMO and therefore aromaticity among the studied compounds which confirms the result of molecular orbital examination.
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15

Dudhe, Anshu R., Sachinkumar D. Gunjal, Sampath AG, Sushama Rawat, and YY Nandurkar. "An Overview on Nitrogen-containing Heterocyclic Compounds as Anticancer Agents." INTERNATIONAL JOURNAL OF PHARMACEUTICAL QUALITY ASSURANCE 14, no. 04 (December 25, 2023): 1296–301. http://dx.doi.org/10.25258/ijpqa.14.4.72.

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Cancer accounts for nearly 10 million losses each year. Among the most prevalent cancer types are breast, lung, colon, rectum, and prostate cancers. Astonishingly, around one-third of cancer-related deaths can be attributed to factors such as tobacco usage, a high body mass index (BMI), alcohol consumption, restricted ingestion of fruits and vegetables, and inadequate bodily bustle. In the field of pharmaceuticals, heteroatoms and heterocyclic compounds frequently assume crucial roles and serve as common structural components in numerous active natural products. Statistically, the majority of biologically active compounds is either heterocycles themselves or incorporate a heterocyclic element, with nitrogen-containing heterocycles being the most prevalent structural framework in these intricate molecules. These findings underscore the significant and ever-evolving role of heterocycles in contemporary drug blueprints and drug sighting practice. The chief hub of the review was to explore the documented anti-cancer properties of nitrogen-containing heterocyclic compounds, as reported in current scientific literature.
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16

Moskalik, Mikhail Yu. "Monofluoromethylation of N-Heterocyclic Compounds." International Journal of Molecular Sciences 24, no. 24 (December 18, 2023): 17593. http://dx.doi.org/10.3390/ijms242417593.

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The review focuses on recent advances in the methodologies for the formation or introduction of the CH2F moiety in N-heterocyclic substrates over the past 5 years. The monofluoromethyl group is one of the most versatile fluorinated groups used to modify the properties of molecules in synthetic medical chemistry. The review summarizes two strategies for the monofluoromethylation of N-containing heterocycles: direct monofluoromethylation with simple XCH2F sources (for example, ICH2F) and the assembly of N-heterocyclic structures from CH2F-containing substrates. The review describes the monofluoromethylation of pharmaceutically important three-, five- and six-membered N-heterocycles: pyrrolidines, pyrroles, indoles, imidazoles, triazoles, benzothiazoles, carbazoles, indazoles, pyrazoles, oxazoles, piperidines, morpholines, pyridines, quinolines and pyridazines. Assembling of 6-fluoromethylphenanthridine, 5-fluoromethyl-2-oxazolines, C5-monofluorinated isoxazoline N-oxides, and α-fluoromethyl-α-trifluoromethylaziridines is also shown. Fluoriodo-, fluorchloro- and fluorbromomethane, FCH2SO2Cl, monofluoromethyl(aryl)sulfoniummethylides, monofluoromethyl sulfides, (fluoromethyl)triphenylphosphonium iodide and 2-fluoroacetic acid are the main fluoromethylating reagents in recent works. The replacement of atoms and entire functional groups with a fluorine atom(s) leads to a change and often improvement in activity, chemical or biostability, and pharmacokinetic properties. The monofluoromethyl group is a bioisoster of -CH3, -CH2OH, -CH2NH2, -CH2CH3, -CH2NO2 and -CH2SH moieties. Bioisosteric replacement with the CH2F group is both an interesting task for organic synthesis and a pathway to modify drugs, agrochemicals and useful intermediates.
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17

Ābele, E., R. Ābele, Ļ. Golomba, J. Višņevska, T. Beresņeva, and K. Rubina. "Oximes of Seven-Membered Heterocyclic Compounds Containing One Heteroatom." Latvian Journal of Chemistry 50, no. 3-4 (January 1, 2011): 205–22. http://dx.doi.org/10.2478/v10161-011-0071-7.

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Oximes of Seven-Membered Heterocyclic Compounds Containing One Heteroatom Literature data on the synthesis and structure of azepane, oxepane and thiepane oximes were reviewed. Synthesis of novel heterocycles from oximes of seven-membered heterocycles containing one heteroatom were described. Biological activity of oximes of seven-membered heterocycles with one heteroatom was also reviewed.
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18

Ābele, E. "Oximes of Seven-Membered Heterocyclic Compounds Containing Two Heteroatoms." Latvian Journal of Chemistry 51, no. 1-2 (January 1, 2012): 83–92. http://dx.doi.org/10.2478/v10161-012-0005-z.

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Oximes of Seven-Membered Heterocyclic Compounds Containing Two Heteroatoms Literature data concerning the synthesis and structure of diazepane, oxazepane and thiazepane oximes were reviewed. Synthesis of novel heterocycles from the oximes of seven-membered heterocycles containing two heteroatoms was described. Biological activity of oximes of seven-membered heterocycles with two heteroatoms was also reviewed.
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19

Mohareb, Rafat, and Hanaa Hana. "Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activity." Acta Pharmaceutica 58, no. 1 (March 1, 2008): 29–42. http://dx.doi.org/10.2478/v10007-007-0043-3.

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Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activityThe aim of this work was to synthesize steroidal heterocycles and to elucidate the potential role of these compounds as antimicrobial agents. The synthesis of steroidal heterocycles containing the pyrazole, isoxazole, thiazole, pyrane, pyridine, pyridazine, or benzopyrane ring attached to the pregnene nucleus is reported. Progesterone (1) reacts with dimethyl formamide dimethyl acetal to form enamine2. Heterocyclization of2with hydrazines, hydroxylamine, glycine, ethyl acetoacetate or cyanomethylene afforded novel steroidal heterocyclic derivatives. Thein vitroantimicrobial evaluation showed that all synthesized compounds show activity against the used strains of Gram positive bacteria and fungi.
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20

Harith M. Al-ajely. "Synthesis and pharmaceutical applications of Oxazine compounds derived from Pyronic, Salicylic, Antharanilic acids and Phenols." International Journal of Science and Research Archive 2, no. 2 (May 30, 2021): 074–86. http://dx.doi.org/10.30574/ijsra.2021.2.2.0250.

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It is well known from FDA reports that More than 75% of the heterocyclic compounds are drugs and 90 of heterocyclic compounds are cancer drugs. The nitrogen-based heterocycles occupy an exclusive position as a valuable source of therapeutic agents in medicinal chemistry. Most drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties, More over heterocyclic compounds are important class of organic chemistry due to their widely spread in nature. Also there are many route for their action and many mechanistic pathways for their preparation and different metabolic actions. This comes from the easily building or removal of any functional group within the molecules. Changing just on group cause to change the metabolic pathway of the drug action and site of attack of the desired target accordingly. This great characteristic value make them much more important in drug discovery programs of many researchers and also encouraged us and drew attentions of other researchers to develop new ways for their synthesis. As a result different pharmacological and medical applications. Oxazie compounds are sub branch of heterocyclic compounds. These compounds having two hetero atoms, Oxygen and nitrogen within their structures make them much more important toward therapeutic studies. We are here in our investigation will focus on the methodologies and the therapeutic action of the titled compounds as well as other various applications.
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21

Talbi, Soumaya, Mustapha Dib, Latifa Bouissane, Hafid Abderrafia, Souad Rabi, and Mostafa Khouili. "Recent Progress in the Synthesis of Heterocycles based on 1,3-diketones." Current Organic Synthesis 19, no. 2 (March 2022): 220–45. http://dx.doi.org/10.2174/1570179418666211011141428.

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: N,O-heterocycles containing the dicarbonyl ring play a significant role in heterocyclic and therapeutic chemistry. Since the discovery of 1,3-diketones, numerous research works have been achieved regarding the synthesis and its chemical reactivity. In this review, we have described the most relevant publications involving β-diketone compounds published during the period between 2018 to date. In addition, we include the 1,3-diketones-based heterocyclic compounds prepared by various synthetic methodologies.
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22

Sharma, Praveen Kumar, Andleeb Amin, and M. Kumar. "Synthetic Methods of Medicinally Important Heterocycles-thiazines: A Review." Open Medicinal Chemistry Journal 14, no. 1 (September 14, 2020): 71–82. http://dx.doi.org/10.2174/1874104502014010071.

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Heterocyclic compounds containing N and S atoms have unique properties so that they can be used as potential reactive materials in pharmacokinetic systems. In medicinal chemistry, the therapeutic applications of nitrogen sulphur heterocycles are well known. Especially, Thiazines attract the attention of chemists due to their great bioactive behavior. The present study is a review of the work carried out by the research community for the synthesis of novel, effective, medicinally important heterocyclic compounds-thiazines.
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23

Hanusek, Jiří, and Vladimír Macháček. "Intramolecular base-catalyzed reactions involving interaction between benzene nitro groups and ortho carbon chains." Collection of Czechoslovak Chemical Communications 74, no. 5 (2009): 811–33. http://dx.doi.org/10.1135/cccc2008216.

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The review is focused on the understanding of processes involving chemical interaction between benzene nitro group and ortho carbon chain containing heteroatom (N, O, S) adjacent to the ring. In most cases these compounds undergo base-catalyzed cyclization to give heteroaromatic N-oxides that can be subsequently transformed to related heterocycles under the same conditions. However, in some cases, depending on substitution of the benzene ring, side chain or the base used, the formation of other compounds – both heterocyclic and non-heterocyclic such as nitroso and azoxy compounds, spiro Meisenheimer adducts – is observed. Review with 31 references.
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24

Deep, Aman, PrachI, and Hament Panwar. "THE CHEMISTRY OF HEALING: HETEROATOMIC DERIVATIZATION AND THEIR MEDICINAL APPLICATIONS." Annals of Science and Allied Research 2, no. 1 (June 30, 2024): 26–37. https://doi.org/10.5281/zenodo.12599903.

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Heterocyclic compounds are gaining attention for their medical and biological applications, with over 90% of new drugs containing them. Among all the heterocyclic molecules, mimics of nitrogen-based heterocycles occupy an exclusive position as a valuable source of therapeutic agents in medicinal chemistry. More than 75% of drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties. In the forthcoming decade, a much greater share of new nitrogen-based pharmaceuticals is anticipated. Many new nitrogen-based heterocycles have been designed. The number of novel N-heterocyclic moieties with significant physiological properties and promising applications in medicinal chemistry is ever-growing. In the present investigation, we amalgamate isatin and several aromatic aldehydes to produce a few thiazolidinone derivatives. This synthesis aims to contribute to the ongoing progress in the development of innovative nitrogen-containing heterocycles.
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25

Soni, Vatsala, Meenakshi Sharma, Vandana Singh, Vaishali Soni, and Kishore D. "Comprehensive Study of Biological Aspects of Heteroring Annelated Benzothiazoles." International Journal of Science, Engineering and Management 9, no. 6 (June 13, 2022): 1–6. http://dx.doi.org/10.36647/ijsem/09.06.a001.

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Heterocyclic chemicals are chemical structures which include at least a single carbon molecule plus at least one other element, such as sulphur, oxygen, or nitrogen, within the ring structure. Benzothiazoles are discussed in terms of synthesis methodologies, structural changes, chemical reactivity, and possible pharmaceutical effectiveness. This research relied upon secondary data obtained from the sources. The qualitative method was used to provide a section of such an evaluation which looked flawless and accurate. A handy methodology strategy is used in inquiry research. Heterocyclic compounds have been widely exploited in bioorganic and medical research for medication development. Scientists are interested in such compounds because of their various physicochemical and pharmacological properties. Recognizing heterocycles is advantageous in both industrial and biological processes. Benzothiazole, a molecular heterocyclic structure, is being studied as a candidate for such creation of larger, often medicinal chemicals. It is highly durable due to its aromatic components; however, it has reactive services that offer the synthesis method. The benzothiazole ring becomes an important framework for the production of colours used throughout the identification of lanthanide metal cations in aqueous environments. This identical basic N, S heterocycle, benzothiazoles, seems to be abundant; for example, it is required essential thiamine action (vitamin B1). Thiazole compounds could also be discovered in medications such as Nosiheptide. This chemistry group is used for about simply for antibacterial purposes; its distinctive heteroring linked derivatives have attracted the curiosity of scientists due to their various biological or indeed medicinal properties.
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26

Charushin, V. N., E. V. Verbitskiy, O. N. Chupakhin, D. V. Vorobyeva, P. S. Gribanov, S. N. Osipov, A. V. Ivanov, et al. "The chemistry of heterocycles in the 21st century." Russian Chemical Reviews 93, no. 7 (July 2024): RCR5125. http://dx.doi.org/10.59761/rcr5125.

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The chemistry of heterocyclic compounds has traditionally been and remains a bright area of chemical science in Russia. This is due to the fact that many heterocycles find the widest application. These compounds are the key structural fragments of most drugs, plant protection agents. Many natural compounds are also derivatives of heterocycles. At present, more than half of the hundreds of millions of known chemical compounds are heterocycles. This collective review is devoted to the achievements of Russian chemists in this field over the last 15–20 years. The review presents the achievements of leading heterocyclists representing both RAS institutes and university science. It is worth noting the wide scope of the review, both in terms of the geography of author teams, covering the whole of our large country, and in terms of the diversity of research areas. Practically all major types of heterocycles are represented in the review. The special attention is focused on the practical applications of heterocycles in the design of new drugs and biologically active compounds, high-energy molecules, materials for organic electronics and photovoltaics, new ligands for coordination chemistry, and many other rapidly developing areas. These practical advances would not be possible without the development of new fundamental transformations in heterocyclic chemistry.&lt;br&gt; Bibliography — 2237 references.
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27

Shah, Pranay, R. I. Patel, and P. J. Vyas. "Preparation and Biological Screening of Novel Heterocyclic Compounds." International Journal of Trend in Scientific Research and Development Volume-3, Issue-3 (April 30, 2019): 632–36. http://dx.doi.org/10.31142/ijtsrd22815.

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28

Mohan, Rahul Sopan, and Deepak Kumar Birla Dr. "The Interactions between Heterocyclic Compounds and Target Proteins Involved with Cancer." International Multispecialty Journal of Health (IMJH) 10, no. 12 (December 31, 2024): 05–13. https://doi.org/10.5281/zenodo.14910256.

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<strong><em>Abstract</em></strong><strong>&mdash;</strong> <em>Cancer is the second leading cause of mortality globally. The World Health Organization forecasts that by 2030, there will be 22 million new cases of cancer globally. Extensive global research focuses on cancer prevention, diagnosis, and treatment procedures. The metabolic profile of cancer cells is distinct from that of normal cells, attributable to epigenetic and genetic abnormalities. Numerous anti-cancer drugs available commercially feature heterocycles as their main structural element. Furthermore, anticancer drugs approved by the FDA from 2010 to 2015 contain heterocyclic rings in their chemical structure. Their extensive cellular processes and mechanisms, along with their prevalence in nature, account for their inclusion in anti-cancer medications. This study elucidates several heterocyclic compounds exhibiting anticancer effects on various cell lines. These compounds feature rings composed of nitrogen, sulfur, and oxygen. The collection of information on heterocyclic rings may facilitate the discovery of novel compounds with potential anticancer properties in the future</em><em>.</em>
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29

Orzeszko, Barbara, Tomasz Świtaj, Anna B. Jakubowska-Mućka, Witold Lasek, Andrzej Orzeszko та Zygmunt Kazimierczuk. "Tumor Necrosis Factor-α Production-Enhancing Properties of Novel Adamantylalkylthio Derivatives of Some Heterocyclic Compounds". Zeitschrift für Naturforschung B 60, № 4 (1 квітня 2005): 471–75. http://dx.doi.org/10.1515/znb-2005-0419.

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Certain adamantylated heterocycles were previously shown to enhance the secretion of tumor necrosis factor alpha (TNF-α) by murine melanoma cells that have been transduced with the gene for human TNF-α and constitutively expressed this cytokine. The stimulatory potency of those compounds depended, among other factors, on the structure of the linker between the adamantyl residue and the heterocyclic core. In the present study, a series of (1-adamantyl)alkylsulfanyl derivatives of heterocyclic compounds was prepared by alkylation of the corresponding thioheterocyles. Of the novel adamantylalkylthio compounds tested in the aforementioned cell line, 2-(2-adamantan-1-ylethylsulfanyl)- 4-methyl-pyrimidine was found to be the most active
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30

Sajida. Munadi. Th.AL-Suraify and Mohammed Abdul-Mounther Othman. "Synthesis and study of spectrally diagnosed heterocyclic compound." International Journal of Research in Pharmaceutical Sciences 11, SPL4 (December 21, 2020): 2613–22. http://dx.doi.org/10.26452/ijrps.v11ispl4.4527.

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In general terms, medicinal chemistry manages the revelation &amp; plan of recent remedial synthetic concoctions &amp; its uses as meds. Throughout the most recent couple of decades, mixes bearing heterocyclic cores have gotten considerably more consideration of the scientific expert, because of their expansive chemo remedial exercises, for example, calming, anthelmintic, hostile to tubercular, against parasitic &amp; hostile to microbial exercises. Furthermore, Heterocycles &amp; medicines are both interred related, the human is totally dependent on drugs &amp; most of the drugs are derived from heterocyclic compounds. Hetero cycles &amp; their derivatives have been excited regards chemist mainly due to broad-spectrum chemical &amp; pharmacological activities. Most of the heterocyclic compounds are naturally occurs &amp; playing the important role of metabolism regards cells of living. There has been a bigger count of pharmacologically attracted compounds of heterocyclic, several of which have been under continues clinical utilization. This paper presented a detailed study of synthesis which is spectrally detected Heterocyclic compounds, in results described the antibacterial activity of (e)-s-4-(is nicotinamide)-5-(phenoxymethyl)-4h-1, 2, 4-triazol-3-yl 3-(substituted phenyl) prop-2- enethioate. (7a-7f) and antifungal activity of (e)-s-4-(isonicotinamido)-5-(phenoxymethyl)-4h-1, 2, 4-triazol-3-yl 3-(substituted phenyl) prop-2-enethioate. (7a-7f), antitubercular activity of against mycobacterium tuberculosis h37rv presented the scope of this paper.
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31

Stepanenko, Sergey A., Danil M. Shivtsov, Anton P. Koskin, Igor P. Koskin, Roman G. Kukushkin, Petr M. Yeletsky, and Vadim A. Yakovlev. "N-Heterocyclic Molecules as Potential Liquid Organic Hydrogen Carriers: Reaction Routes and Dehydrogenation Efficacy." Catalysts 12, no. 10 (October 17, 2022): 1260. http://dx.doi.org/10.3390/catal12101260.

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This study is focused on the development of liquid organic hydrogen carriers (LOHC) based on N-heterocyclic compounds. These LOHC-substrates are attractive for their lower hydrogen extraction temperature compared to cycloalkanes, which is caused by the low enthalpy of the dehydrogenation reaction of the N-heterocyclic compounds. The low hydrogen extraction temperature, as well as the low volatility of the heterocycles, provide high purity hydrogen from the reaction. Under similar reaction conditions, the comparison of the efficacy of three promising heterocycles (1-methyl-octahydroindole (8HMI), tetradecahydrophenazine and decahydroquinoline) was carried out in the presence of palladium-containing catalysts. As a result, the advantages of using catalysts supported by alumina, and the high perspectivity of the 8MHI application as a LOHC-substrate, were shown. The dehydrogenation of 8HMI in the presence of 1 wt.% Pd/Al2O3 allowed for reaching a 100% yield in hydrogen under the conditions of the standard catalytic test (1 h, 240 °C). In order to study the high reactivity of 8HMI, thermodynamic dehydrogenation reaction profiles were computationally evaluated, which showed that 8HMI was the most energetically preferred in the field of hydrogen storage from the studied heterocyclic compounds.
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32

Grinevich, Oksana I., Anastasia Yu Sholokhova, and Dmitriy D. Matyushin. "The retention features of nitrogen-containing heterocyclic compounds in reversed-phase and hydrophilic HPLC-MS modes." Сорбционные и хроматографические процессы 24, no. 3 (July 19, 2024): 373–85. http://dx.doi.org/10.17308/sorpchrom.2024.24/12239.

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Aromatic five- and six-membered nitrogen-containing heterocyclic compounds are biologically active substances and are widely used in biochemistry and medicine. In addition, such compounds are known as ecotoxicants formed during oxidation processes in industrial wastewater. High-performance liquid chromatography-mass spectrometry is widely used to determine nitrogen-containing heterocycles in various complex mixtures. Octadecyl silica gel is the main sorbent for chromatographic separation. However, octadecyl silica gel does not always enable satisfactory separation in the presence of highly polar isomeric molecules, and more selective chromatographic approaches are required. One of these is hydrophilic chromatography, which facilitates the separation of polar compounds. The aim of the study was to comparatively characterize the retention of a number of five- and six-membered nitrogen-containing heterocyclic compounds during reversed-phase and hydrophilic liquid chromatography with mass spectrometric detection. In addition, spectrophotometric detection at a wavelength of 210 nm was carried out. In the study, we used sorbents based on octadecyl silica gel and unmodified silica gel. High-resolution mass spectrometry was used in the electrospray ionization mode. We studied 19 nitrogen-containing heterocyclic compounds. We used aqueous acetonitrile mobile phases with added aqueous solutions of formic acid and diethylamine as acid-base modifiers. An ammonium formate solution was used as a modifier during hydrophilic chromatography. Reversed-phase chromatography showed that the introduction of 0.1% aqueous formic acid solution increased the ionization and the mass spectrometer signal intensity, but did not always result in a satisfactory separation of isomers upon elution from the octadecyl silica gel surface. The introduction of 0.01% diethylamine solution provided no significant improvement in the separation compared to the mobile phase without modifiers. The use of unmodified silica gel in hydrophilic chromatography mode allowed us to separate isomeric five-membered heterocycles, which was demonstrated by narrow symmetric peaks, but did not result in selective separation of isomeric diazines. Thus, we studied the retention of 19 nitrogen-containing heterocyclic compounds using reversed-phase and hydrophilic liquid chromatography with electrospray ionisation. It was determined that hydrophilic chromatography on unmodified silica gel could be used for satisfactory separation of isomeric five-membered heterocyclic compounds of different classes. For six-membered heterocycles, satisfactory separation was achieved by elution from the surface of octadecyl silica gel using aqueous acetonitrile mobile phase without modifiers.
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33

Monier, Mohamed, Doaa Abdel-Latif, Ahmed El-Mekabaty, Başak D. Mert, and Khaled M. Elattar. "Advances in the Chemistry of 6-6 Bicyclic Systems: Chemistry of Pyrido[3,4- d]pyrimidines." Current Organic Synthesis 16, no. 6 (November 26, 2019): 812–54. http://dx.doi.org/10.2174/1570179416666190704113647.

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The aim of this work is to discuss the chemistry of pyrido[3,4-d]pyrimidines as one of the most important heterocyclic compounds with remarkable synthetic, biological and medical applications. In this overview, the chemistry of heterocyclic compounds incorporated the pyrido[3,4-d]pyrimidine scaffold as demonstrated by chemical reactions and different preparation processes. The anticipated compounds were synthesized from pyridine or pyrimidine compounds and a description of the reactivity of substituents attached to ring carbon and nitrogen atoms is discussed. On the other hand, the synthesis and reactions of fused heterocycles incorporated pyrido[3,4-d]pyrimidine scaffold is described. The diamine analogs included pyrido[3,4-d]pyrimidine core were reported as tyrosine kinase inhibitors. The chemical reactions of certain unexpected and chemically substantial compounds have been discussed.
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34

Chambers, Richard D., Mohammed A. Hassan, Philip R. Hoskin, Alan Kenwright, Paul Richmond, and Graham Sandford. "Polyhalogenated heterocyclic compounds." Journal of Fluorine Chemistry 111, no. 2 (October 2001): 135–46. http://dx.doi.org/10.1016/s0022-1139(01)00445-6.

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35

Benmansour, Hadjar, Richard D. Chambers, Graham Sandford, Graham McGowan, Slimane Dahaoui, Dmitrii S. Yufit, and Judith A. K. Howard. "Polyhalogenated heterocyclic compounds." Journal of Fluorine Chemistry 112, no. 2 (December 2001): 349–54. http://dx.doi.org/10.1016/s0022-1139(01)00534-6.

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36

Chambers, Richard D., Ali Khalil, Christopher B. Murray, Graham Sandford, Andrei S. Batsanov, and Judith A. K. Howard. "Polyhalogenated heterocyclic compounds." Journal of Fluorine Chemistry 126, no. 7 (July 2005): 1002–8. http://dx.doi.org/10.1016/j.jfluchem.2005.01.018.

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37

Pooja Rani. "Multicomponent synthesis of heterocyclic compounds." International Journal for Research Publication and Seminar 11, no. 3 (September 30, 2020): 223–33. http://dx.doi.org/10.36676/jrps.v11.i3.1184.

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Rapid and efficient, multicomponent domino reactions (MDRs) are a useful tool for the one-pot synthesis of flexible heterocycles with diverse and complicated structures. Reduced chemical waste, lower starting-material prices, and lower energy and labour requirements are all possible thanks to these reactions. Additionally, the time required for a response may be greatly reduced. The most up-to-date research on multicomponent domino reactions for constructing heterocyclic skeletons with five, six, or seven members, as well as their multicyclic derivatives, is discussed in this Review. In recent years, our group has developed innovative procedures based on the transition-metal-mediated intramolecular addition reaction of heteronucleophiles and stabilised carbon nucleophiles to inactivated alkenes and alkynes. We provide a brief overview of many recent synthetic uses of these novel methods in this paper. Multicomponent reactions involving Pd-mediated intramolecular cyclization followed by carbon-carbon bond formation are the focus here.
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38

Drapak, І. V. "In silico screening of drug-like molecules for the treatment of cardiovascular diseases on the basis of five-membered privileged heterocycles." Farmatsevtychnyi zhurnal, no. 4 (September 10, 2019): 61–72. http://dx.doi.org/10.32352/0367-3057.4.19.07.

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Among various heterocyclic systems, the derivatives of five-membered heterocycles are of special interest. Most of the above mentioned heterocycles are treatred as so-called privileged structures in modern medicinal chemistry. In silico screening among five-membered heterocycles of molecules for the treatment of cardiovascular diseases is actual.&#x0D; The aim of the work was the search for synthetic drug-like molecules based on functionalized five-membered heterocycles and related heterocyclic systems as an element of the theoretical platform for rational design of compounds acting on the cardiovascular system, and prediction of their possible mechanism of action.&#x0D; The objects of the study were derivatives of uncondensed and condensed five-membered heterocycles. In the work, in silico approaches were applied using the programs: Hyper-Chem, PASS, AutoDock, PROTOX.&#x0D; Based on the previous studies, focused sub-libraries of small synthetic drug-like molecules based on functionalized five-membered heterocycles and related heterocyclic systems have been selected. The compounds were divided on 12 groups. The optimization of the compound structures, the drug-like parameters calculation were carried out. The activity prediction, the acute toxicity level and docking studies to probable bio-targets which are related with cardiovascular drug mechanism of action have been carried out. It was shown that thiazole and thiadiazole based compounds possessed the highest calculated affinity levels to selected bio-targets. This is consistent with PASS-based prediction data.&#x0D; Diverse functionalized derivatives of five-membered heterocycles (thiazole, thiazolidine, thiadiazole, pyrazole, thiophene, triazole) and related fused heterocycles have been grouped in focused sub-libraries of compounds. it has been established that thiazole and thiadiazole based compounds are promising objects for directed synthesis and further modification as potential cardiovascular agents based on the prediction of biological activity, the calculation of affinity to potent bio-targets, and the prediction of the drug-like features and acute toxicity level. The prognostic values of the parameters of the above mentioned groups of compounds may be used as the element of theoretical platform for the search and de novo design of potential drugs for the treatment of cardiovascular diseases.
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39

Cui, Hai-Lei. "Recent Advances in DMSO-Based Direct Synthesis of Heterocycles." Molecules 27, no. 23 (December 2, 2022): 8480. http://dx.doi.org/10.3390/molecules27238480.

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Besides serving as a low-toxicity, inexpensive and easily accessible solvent, dimethyl sulfoxide (DMSO) has also been extensively used as a versatile reagent for the synthesis of functionalized molecules. Dimethyl sulfoxide can not only be utilized as a carbon source, a sulfur source and an oxygen source, but also be employed as a crucial oxidant enabling various transformations. The past decade has witnessed a large number of impressive achievements on the direct synthesis of heterocycles as well as modifications of heterocyclic compounds by applying DMSO as a reagent. This review summarized the DMSO-based direct heterocycle constructions from 2012 to 2022.
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40

Ibragimova, Mahliyo. "ANALYSIS OF HETEROCYCLIC COMPOUNDS." "Science and innovation" international scientific journal. ISSN: 2181-3337 1, no. 4 (August 8, 2022): 266–65. https://doi.org/10.5281/zenodo.6973947.

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<em>This article describes heterocyclic compounds and the classification of their structure. Each atom of an element with two or more valences can participate in the formation of heterocyclic compounds. But among them, the most stable, widespread, well studied and important are heterocyclic compounds containing nitrogen, oxygen and sulfur. The reason for the formation of ring compounds with these atoms and carbon atoms is that the bond angles in the compounds of these atoms are very close to the bond angles of the hybridized C atom (sp 3 hybridization &alpha;=1090 and sp 2 hybridization &alpha;=1200).</em>
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41

Depa, Navaneetha, and Harikrishna Erothu. "SYNTHESIS AND BIOLOGICAL ACTIVE COMPOUNDS OF NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS: A REVIEW." RASAYAN Journal of Chemistry 15, no. 03 (2022): 1709–17. http://dx.doi.org/10.31788/rjc.2022.1536924.

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Heterocyclic chemistry has a broad spectrum of applications in our day-to-day life. Heterocyclic compounds contain hetero atoms like oxygen, nitrogen, and sulphur in their structure. Among these atoms, a wide variety of heterocyclic moieties with nitrogen as hetero atoms have considerable physiological properties and useful medical applications. Nitrogen-containing heterocyclic compounds are considered a significant category due to their broad therapeutic applications like antibacterial, antimalarial, anticancer, antifungal, anti-HIV, anti-inflammatory, etc., this review article focuses on novel moieties of indole, pyrazole, and triazole compounds and its biological importance
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42

Puranik, Nidhi, and Minseok Song. "Therapeutic Role of Heterocyclic Compounds in Neurodegenerative Diseases: Insights from Alzheimer’s and Parkinson’s Diseases." Neurology International 17, no. 2 (February 7, 2025): 26. https://doi.org/10.3390/neurolint17020026.

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Alzheimer’s and Parkinson’s are the most common neurodegenerative diseases (NDDs). The development of aberrant protein aggregates and the progressive and permanent loss of neurons are the major characteristic features of these disorders. Although the precise mechanisms causing Alzheimer’s disease (AD) and Parkinson’s disease (PD) are still unknown, there is a wealth of evidence suggesting that misfolded proteins, accumulation of misfolded proteins, dysfunction of neuroreceptors and mitochondria, dysregulation of enzymes, and the release of neurotransmitters significantly influence the pathophysiology of these diseases. There is no effective protective medicine or therapy available even with the availability of numerous medications. There is an urgent need to create new and powerful bioactive compounds since the number of people with NDDs is rising globally. Heterocyclic compounds have consistently played a pivotal role in drug discovery due to their exceptional pharmaceutical properties. Many clinically approved drugs, such as galantamine hydrobromide, donepezil hydrochloride, memantine hydrochloride, and opicapone, feature heterocyclic cores. As these heterocyclic compounds have exceptional therapeutic potential, heterocycles are an intriguing research topic for the development of new effective therapeutic drugs for PD and AD. This review aims to provide current insights into the development and potential use of heterocyclic compounds targeting diverse therapeutic targets to manage and potentially treat patients with AD and PD.
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43

Nehra, Bhupender, Bijo Mathew, and Pooja A. Chawla. "A Medicinal Chemist’s Perspective Towards Structure Activity Relationship of Heterocycle Based Anticancer Agents." Current Topics in Medicinal Chemistry 22, no. 6 (March 2022): 493–528. http://dx.doi.org/10.2174/1568026622666220111142617.

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Aim: This paper aims to describe the structure activity relationship of heterocyclic deriva-tives with multi-targeted anticancer activity. Objectives: With the following goals in mind, this review tries to describe significant recent advances in the medicinal chemistry of heterocycle-based compounds: (1) To shed light on recent literature focused on heterocyclic derivatives' anticancer potential; (2) To discuss recent advances in the medic-inal chemistry of heterocyclic derivatives, as well as their biological implications for cancer eradica-tion; (3) To summarise the comprehensive correlation of structure activity relationship (SAR) with pharmacological outcomes in cancer therapy. Background: Cancer remains one of the major serious health issues in the world today. Cancer is a complex disease in which improperly altered cells proliferate at an uncontrolled, rapid, and severe rate. Variables such as poor dietary habits, high stress, age, and smoking, can all contribute to the development of cancer. Cancer can affect almost any organ or tissue, although the brain, breast, liver, and colon are the most frequently affected organs. For several years, surgical operations and irradia-tion have been in use along with chemotherapy as a primary treatment of cancer, but still, effective treatment of cancer remains a huge challenge. Chemotherapy is now considered one of the most ef-fective strategies to eradicate cancer, although it has been shown to have a number of cytotoxic and unfavourable effects on normal cells. Despite all of these cancer treatments, there are several other targets for anticancer drugs. Cancer can be effectively eradicated by focusing on these targets, includ-ing cell-specific and receptor-specific targets such as tyrosine kinase receptors (TKIs). Heterocyclic scaffolds also have a variety of applications in drug development and are a common moiety in the pharmaceutical, agrochemical, and textile industries. Methods: The association between structural activity relationship data of many powerful compounds and their anticancer potential in vitro and in vivo has been studied. SAR of powerful heterocyclic compounds can also be generated using molecular docking simulations, as reported in literature. Conclusions: Heterocycles have a wide range of applications, from natural compounds to synthesised derivatives with powerful anticancer properties. To avoid cytotoxicity or unfavourable effects on normal mammalian cells due to a lack of selectivity towards the target site, as well as to reduce the occurrence of drug resistance, safer anticancer lead compounds with higher potency and lower cyto-toxicity are needed. This review emphasizes on design and development of heterocyclic lead com-pounds with promising anticancer potential.
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44

Francke, Robert. "Recent advances in the electrochemical construction of heterocycles." Beilstein Journal of Organic Chemistry 10 (December 3, 2014): 2858–73. http://dx.doi.org/10.3762/bjoc.10.303.

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Due to the fact that the major portion of pharmaceuticals and agrochemicals contains heterocyclic units and since the overall number of commercially used heterocyclic compounds is steadily growing, heterocyclic chemistry remains in the focus of the synthetic community. Enormous efforts have been made in the last decades in order to render the production of such compounds more selective and efficient. However, most of the conventional methods for the construction of heterocyclic cores still involve the use of strong acids or bases, the operation at elevated temperatures and/or the use of expensive catalysts and reagents. In this regard, electrosynthesis can provide a milder and more environmentally benign alternative. In fact, numerous examples for the electrochemical construction of heterocycles have been reported in recent years. These cases demonstrate that ring formation can be achieved efficiently under ambient conditions without the use of additional reagents. In order to account for the recent developments in this field, a selection of representative reactions is presented and discussed in this review.
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45

Asif, Mohammad. "Biological Potential and Chemical Properties of Pyridine and Piperidine Fused Pyridazine Compounds: Pyridopyridazine a Versatile Nucleus." Asian Journal of Chemistry and Pharmaceutical Sciences 1, no. 1 (November 21, 2016): 29. http://dx.doi.org/10.18311/ajcps/2016/7693.

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Pyridopyridazine compounds are important nitrogen atom containing heterocyclic compounds due to their pharmacological versatility. This heterocycle system characterized a structural feature for different types of bioactive compounds that exhibiting various types of biological activities which make it an attractive scaffold for the design and development of new drug molecules. This article provided information about the pharmacological properties of pyridopyridazines derivatives.
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46

Gaonkar, Santosh L., Vignesh U. Nagaraj, and Swarnagowri Nayak. "A Review on Current Synthetic Strategies of Oxazines." Mini-Reviews in Organic Chemistry 16, no. 1 (November 19, 2018): 43–58. http://dx.doi.org/10.2174/1570193x15666180531092843.

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In the past three decades, the heterocyclic oxazine cores have been intensely concerned. Oxazine derivatives are promising vital heterocyclic motifs. They are eminent for their synthetic potential and extensive biological properties. Oxazines are versatile intermediates for the synthesis of a variety of heterocycles and bifunctional compounds. Researchers have reported several synthetic approaches for the preparation of oxazines. This review emphasises the recent approaches for the synthesis of oxazine derivatives.
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47

Su, Biyun, Yifan Hou, Li Wang, Xiaoteng Li, Dandan Pan, Tingyu Yan, Ao Zhang, Faida Paison та Liqing Ding. "The Syntheses, Characterization and Crystal Structures of a Series of Heterocyclic β-Diketones and Their Isoxazole Compounds". Current Organic Synthesis 16, № 8 (20 січня 2020): 1174–84. http://dx.doi.org/10.2174/1570179416666191022113022.

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Background: In the field of coordination chemistry, the introduction of heterocyclic substituents into the structure of β-diketone enables ligand to produce multiple coordination sites. The adoption of small steric oxime group into the structure of heterocyclic β-diketone by Schiff-base condensation will further increase coordination sites and facilitate the generation of polynuclear structures. Objective: A series of β-diketones (2a-2c) containing different heterocycles such as pyridine, thiophene and furan and their corresponding isoxazole compounds (3a-3c) were synthesized. Materials and Methods: The Claisen condensations were investigated in a solvent-free rheological phase system at room temperature to obtain heterocyclic β-diketones 2a-2c, which further reacted with hydroxylamine hydrochloride to obtain heterocyclic isoxazoles 3a-3c. All these compounds were well characterized by EA, IR, 1H NMR and X-ray crystal diffraction to confirm the structures. Synthetic mechanisms of compounds and the effects of different heterocycles on reactivity were discussed deeply. Result: 1H NMR indicated that these β-diketones do not exist as a total diketonic form but an equilibration between diketone and enol forms in CDCl3 solvent, in which the enol form accounts for 98.0% in 2a, 94.3% in 2b, 95.5% in 2c. While the crystal structures of 2a-2c showed that the reaction allows to isolate diketones in solid state. Crystal structures of 3a-3c showed that the neutral β-ketone oximes resonate and cyclize to form the target heterocyclic isoxazoles. Conclusion: SN1 nucleophilic substitution mechanism of Claisen ketoester condensation was proposed for the syntheses of 2a-2c, and SN1 single molecule nucleophilic substitution reaction mechanism was put forward for 3a-3c.
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48

Mir, Reyaz Hassan, Prince Ahad Mir, Roohi Mohi-ud-din, Saba Sabreen, Mudasir Maqbool, Abdul Jalil Shah, Kitika Shenmar, Syed Naeim Raza, and Faheem Hyder Pottoo. "A Comprehensive Review on Journey of Pyrrole Scaffold against Multiple Therapeutic Targets." Anti-Cancer Agents in Medicinal Chemistry 22 (June 13, 2022). http://dx.doi.org/10.2174/1871520622666220613140607.

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Abstract: Heterocyclic compounds are that type of substances that are deeply intertwined with biological processes. Heterocycles are found in about 90% of commercially available medicines. In medicinal chemistry, finding new synthetic molecules with drug-like characteristics is a regular problem, which triggered the development of pharmacological molecules, the majority of which are based on N-heterocyclic motifs. Among the heterocycles, the pyrrole scaffold is the most commonly found heterocycle in both natural and synthetic bioactive compounds. Pyrrole has a five-membered heterocyclic ring with a plethora of pharmacophores, resulting in a library of different lead compounds. Pyrrole derivatives are physiologically active heterocyclic compounds that can be used as scaffolds for antibacterial, antiviral, anticancer, antitubercular, anti-inflammatory, and as enzyme inhibitors. On account of its extensive pharmacological profile, pyrrole and its various synthetic derivatives have drawn much attention among researchers to explore it for the benefit of humankind. This review presents an overview of recent developments in the pyrrole derivatives against multiple therapeutic targets.
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Devi, Ahanthem Priyanca, Andrea Penoni, Vnira R. Akhmetova, Rajendra P. Pawar, Is Fatimah, and Keshav Lalit Ameta. "An Overview of Palladium-Catalyzed Fabrication of Some Heterocyclic Frameworks." Mini-Reviews in Organic Chemistry 19 (June 15, 2022). http://dx.doi.org/10.2174/1570193x19666220615095645.

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Abstract: Heterocycles are the largest family of organic compounds due to their wide applications as therapeutic agents, synthetic intermediates, scaffolds, building blocks or fine chemicals. Heterocyclic compounds are continuously used in material science, biotechnology, pharmaceutical and agrochemical industries. In the past few years, the use of transition metal complexes especially palladium as a heterogeneous catalyst has become a trend for the synthesis of various organic compounds. Pd-catalyzed reactions have proven to be effective ways for synthesising a variety of heterocyclic compounds, which are a popular class of molecules in chemical study. Hence, in this review we have discussed the palladium catalyzed synthesis of various heterocyclic compounds i,e. furan, indole, quinoline, coumarin and some other heterocycle derivatives.
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Zeki, Nameer Mazin, and Yasser Fakri Mustafa. "Annulated Heterocyclic[g]Coumarin Composites: Synthetic Approaches and Bioactive Profiling." Chemistry & Biodiversity, December 25, 2023. http://dx.doi.org/10.1002/cbdv.202301855.

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Coumarins, widely abundant natural heterocyclic compounds, are extensively employed in creating various biologically and pharmacologically potent substances. The hybridization of heterocycles presents a key opportunity to craft innovative multicyclic compounds with enhanced biological activity. Fusing different heterocyclic rings with the coumarin structure presents an intriguing method for crafting fresh hybrid compounds possessing remarkable biological effects. In the pursuit of creating heterocyclic‐fused coumarins, a wide range of annulated heterocyclic[g]coumarin composites has been introduced, displaying impressive biological potency. The influence of the linear attachment of heterocyclic rings to the coumarin structure on the biological performance of the resulting compounds has been investigated. This review centers on the synthetic methodologies, structural activity relationship investigation, and biological potentials of annulated heterocyclic[g]coumarin composites. We conducted searches across several databases, including Web of Science, Google Scholar, PubMed, and Scopus. After sieving, we ultimately identified and included 71 pertinent studies published between 2000 and the middle of 2023. This will provide valuable perspectives for medicinal chemists in the prospective design and synthesis of lead compounds with significant therapeutic effects, centered around heterocycle‐fused coumarin frameworks.
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