Journal articles: 'Bioactive heterocyclic compounds'

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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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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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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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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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Sultan Alwan, Ensaf, and Rafat Milad Mohareb. "Synthesis of bioactive heterocyclic compounds using camphor." Bulletin of the Chemical Society of Ethiopia 38, no. 4 (April 30, 2024): 1069–76. http://dx.doi.org/10.4314/bcse.v38i4.20.

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The aim of the work was to synthesize novel heterocyclic compounds derived from camphor with antibacterial activity. The pyridazine, xanthene, pyranothiazole, pyridinothiazole, thiophene and pyrazole derivatives were produced from 4,11,11-trimethyl-9-phenyl-7-(2-phenylhydrazono)-3,4,5,6,7,9-hexahydro-1H-1,4-methanoxanthen-8(2H)-one (1). Thiophene derivatives 6a,b were produced according to the Gewald’s reaction for thiophene synthesis. On the other hand, pyranothiazol derivatives 8a,b were synthesized by the multicomponent reactions between xanthene derivative 5, benzaldehyde and ethylcyanoacetate or malononitrile in ethanol/triethylamine. Whereas, pyridinothiazole derivative 9 was produced in ethanol/ammonium acetate by the multicomponent reaction between xanthene derivative 5, benzaldehyde and malononitrile. The antibacterial activity of the synthesized compounds was evaluated against E. coli bacteria. All synthesized compounds showed moderate activity against E. coli bacteria. KEY WORDS: Anti-microbial, Camphor, Heterocyclic, Pyrazol-3(2H)-one, Thiazol-4(5H)-one, Thieno[3,2-d]thiazole, Xanthenes Bull. Chem. Soc. Ethiop. 2024, 38(4), 1069-1076. DOI: https://dx.doi.org/10.4314/bcse.v38i4.20

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Ge, Tony, and Jean-Christophe Cintrat. "Pyrrolotriazinone as an Underexplored Scaffold in Drug Discovery." Pharmaceuticals 14, no. 12 (December 6, 2021): 1275. http://dx.doi.org/10.3390/ph14121275.

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Heterocyclic amino derivatives have been extensively synthesized and validated as potent bioactive compounds, and nowadays, numerous marketed drugs share these scaffolds, from very simple structures (monoamino, monocyclic compounds) to much more complex molecules (polycyclic derivatives with two or more nitrogen atoms within the (fused) rings). In a constant quest for new chemical entities in drug discovery, a few novel heterocycles have emerged in recent years as promising building blocks for the obtainment of bioactive modulators. In this context, pyrrolotriazinones have attracted attention, and some show promising biological activities. Here, we offer an extensive review of pyrrolo[2,1-f][1,2,4]triazin-4(1H)-one and pyrrolo[1,2-d][1,2,4]triazin-4(3H)-one, describing their biological properties en route to drug discovery.

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Valdomir, Guillermo, María de los Ángeles Fernández, Irene Lagunes, Juan I. Padrón, Víctor S. Martín, José M. Padrón, and Danilo Davyt. "Oxa/thiazole-tetrahydropyran triazole-linked hybrids with selective antiproliferative activity against human tumour cells." New Journal of Chemistry 42, no. 16 (2018): 13784–89. http://dx.doi.org/10.1039/c8nj02388c.

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Bassam A. Hassan, Hameedi N Nasera, and Maitham M. Abdulridha. "Synthesis and antimicrobial evaluation of fused heterocyclic compound [1,2,4] triazolo [4,3-b][1,2,4,5] tetra zine." International Journal of Research in Pharmaceutical Sciences 10, no. 2 (April 14, 2019): 1254–58. http://dx.doi.org/10.26452/ijrps.v10i2.417.

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Nitrogen-containing, heterocycles, have special importance and vital, role in the discovery of effective bioactive, agents in the pharmaceutical, industry. The present article reports the synthesis of new fused, heterocycles triazolotetrazine by cyclo condensation, reaction as shown in scheme(1). The structures formula of synthesized compounds newly was evaluated by Ft-IR,1H-NMR spectrum, and C, H, N elemental analysis. Antimicrobial activity of triazolotetrazine studied against some pathogenic bacterial strains isolated from patients like Acinetobacter, Aeromonas, E. coli, Klebsiella, Staphylococcus, Streptococcus. Eventually, antibacterial of the fused heterocyclic compound was exhibited significant growth inhibition against some pathogenic bacteria which consider an important source of new antimicrobial compounds. The results, of such studies, are discussed in this paper.

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Akishina, E. A., and Е. А. Dikusar. "Chemical modification of different compounds with nitrogen-containing heterocycles." Proceedings of the National Academy of Sciences of Belarus, Chemical Series 57, no. 3 (September 5, 2021): 356–84. http://dx.doi.org/10.29235/1561-8331-2021-57-3-356-384.

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Heterocyclic compounds have an extremely important practical application, since many heterocycles are the basis of the most valuable medicinal substances, both natural (vitamins, enzymes, alkaloids, etc.) and synthetic biologically active compounds. The work mainly considers the most relevant directions for various purposes drugs search by modifying known bioactive natural, organoelement and framework compounds with 1,2-azole, oxazole, oxadiazole, thiazole, triazole, pyridine, pyrimidine heterocycles over the past 10 years. Chemical modification makes it possible to increase the water solubility of the compounds, which is important when choosing the pathways for the most rational drug introduction into the body, to reduce the toxicity of the corresponding substances, to increase the breadth of the therapeutic action, and also to give new valuable medicinal properties, thus significantly expanding their application in medicine and agriculture.

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Karan, Ram, Pooja Agarwal, Mukty Sinha, and Neelima Mahato. "Recent Advances on Quinazoline Derivatives: A Potential Bioactive Scaffold in Medicinal Chemistry." ChemEngineering 5, no. 4 (October 26, 2021): 73. http://dx.doi.org/10.3390/chemengineering5040073.

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This paper intended to explore and discover recent therapeutic agents in the area of medicinal chemistry for the treatment of various diseases. Heterocyclic compounds represent an important group of biologically active compounds. In the last few years, heterocyclic compounds having quinazoline moiety have drawn immense attention owing to their significant biological activities. A diverse range of molecules having quinazoline moiety are reported to show a broad range of medicinal activities like antifungal, antiviral, antidiabetic, anticancer, anti-inflammatory, antibacterial, antioxidant and other activities. This study accelerates the designing process to generate a greater number of biologically active candidates.

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Borah, Biplob, and L. Raju Chowhan. "Ultrasound-assisted transition-metal-free catalysis: a sustainable route towards the synthesis of bioactive heterocycles." RSC Advances 12, no. 22 (2022): 14022–51. http://dx.doi.org/10.1039/d2ra02063g.

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12

Neha, Ashish Ranjan Dwivedi, Rakesh Kumar, and Vinod Kumar. "Recent Synthetic Strategies for Monocyclic Azole Nucleus and Its Role in Drug Discovery and Development." Current Organic Synthesis 15, no. 3 (April 27, 2018): 321–40. http://dx.doi.org/10.2174/1570179414666171013154337.

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Background: In recent years, the development and diversification of heterocyclic compounds has become central to the discovery of bioactive compounds with novel or improved pharmacological properties. In particular, N-containing heterocycles are proved to be promising leads and drug candidates, and received huge attention of the medicinal chemists. Objective: Many drugs especially antibiotics are becoming obsolete due to the development of multidrug resistance. Moreover, toxicity and other side effects of some drugs necessitated the quest for safer and more potent drug candidates. The current review article described biological potential of various monocyclic azoles. Recent developments in the synthesis of azole derivatives have been also reviewed. Conclusion: The presence of N-heterocyclic rings can influence the pharmacokinetics, pharmacodynamics, pKa and bioavailability profile of the drug molecules. Compounds containing monocyclic azole rings showed various biological activities and number of molecules are in clinical practice. A number of important leads and potential drug candidates containing azole nucleus are in advance stages of drug developments. Thus, simple, atom economic and more efficient synthetic strategies are desired for the synthesis of new libraries of the compounds.

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13

Darwish, Yassin, Tibor Cserháti, and Esther Forgács. "Reversed-phase retention characteristics of some bioactive heterocyclic compounds." Journal of Chromatography A 668, no. 2 (May 1994): 485–94. http://dx.doi.org/10.1016/0021-9673(94)80144-4.

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14

Chen, Zhangpei, Lingxin Meng, Zhiqiang Ding, and Jianshe Hu. "Construction of Versatile N-Heterocycles from in situ Generated 1,2-Diaza-1,3-dienes." Current Organic Chemistry 23, no. 2 (April 23, 2019): 164–87. http://dx.doi.org/10.2174/1385272823666190227162840.

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N-Heterocyclic architectures are omnipresent in many bioactive natural products, synthetic drugs, and materials science, thus have evoked a vast research interest of academic, as well as industrial chemists. Recently, several efficient methods have been developed for the preparation of various nitrogen-containing compounds with in situ generated 1,2-diaza-1,3-dienes from the easily available precursors including α -haloketohydrazones, α-hydroxyl ketohydrazones, thiadiazole dioxides or their analogues, and other simple hydrazones. These methods are considered powerful tools in the synthesis of five-, six- and seven-membered ring heterocyclic compounds with good to excellent levels of conversions and selectivities. This review mainly summarizes recent advances on the chemistry of construction of versatile N-heterocycles from in situ generated 1,2-diaza-1,3- dienes and presents an extensive summary of the application scopes and limitations of the corresponding cyclization reactions. Moreover, enantioselective approaches are also covered.

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Rajai-Daryasarei, Saideh, Mohammad Hossein Gohari, and Narges Mohammadi. "Reactions involving aryl methyl ketone and molecular iodine: a powerful tool in the one-pot synthesis of heterocycles." New Journal of Chemistry 45, no. 44 (2021): 20486–518. http://dx.doi.org/10.1039/d1nj03572j.

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The preparation of heterocyclic compounds has attracted great attention in organic chemistry because of their extensive application in the field of bioactive molecules, materials science, and natural products.

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Polshettiwar, Vivek, and Rajender S. Varma. "Greener and expeditious synthesis of bioactive heterocycles using microwave irradiation." Pure and Applied Chemistry 80, no. 4 (January 1, 2008): 777–90. http://dx.doi.org/10.1351/pac200880040777.

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The utilization of green chemistry techniques is dramatically reducing chemical waste and reaction times as has recently been proven in several organic syntheses and chemical transformations. To illustrate these advantages in the synthesis of bioactive heterocycles, we have studied various environmentally benign protocols that involve greener alternatives. Microwave (MW) irradiation of neat reactants catalyzed by the surfaces of recyclable mineral supports, such as alumina, silica, clay, or their "doped" versions, enables the rapid one-pot assembly of heterocyclic compounds, such as flavonoids, related benzopyrans, and quinolone derivatives. The strategy to assemble oxygen and nitrogen heterocycles from in situ generated reactive intermediates via enamines or using hypervalent iodine reagents is described. Examples of multicomponent reactions that can be adapted for rapid parallel synthesis include solventless synthesis of dihydropyrimidine-2(1H)-ones (Biginelli reaction), imidazo[1,2-a]annulated pyridines, pyrazines, and pyrimidines (Ugi reaction). The relative advantages of greener pathways, which use MW irradiation and eco-friendly aqueous reaction medium, for the synthesis of various heterocycles, such as N-aryl azacycloalkanes, isoindoles, 1,3-dioxane, 1,3,4-oxadiazole, 1,3,4-thiadiazole, pyrazole, and diazepines, are also summarized.

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Marzi, Mahrokh, Mojtaba Farjam, Zahra Kazeminejad, Abolfazl Shiroudi, Amin Kouhpayeh, and Elham Zarenezhad. "A Recent Overview of 1,2,3-Triazole-Containing Hybrids as Novel Antifungal Agents: Focusing on Synthesis, Mechanism of Action, and Structure-Activity Relationship (SAR)." Journal of Chemistry 2022 (January 6, 2022): 1–50. http://dx.doi.org/10.1155/2022/7884316.

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A pharmacophore system has been found as 1,2,3-triazole, a five-membered heterocycle ring with nitrogen heteroatoms. These heterocyclic compounds can be produced using azide-alkyne cycloaddition processes catalyzed by ruthenium or copper. The bioactive compounds demonstrated antitubercular, antibacterial, anti-inflammatory, anticancer, antioxidant, antiviral, and antidiabetic properties. This heterocycle molecule, in particular, with one or more 1,2,3-triazole cores has been found to have the most powerful antifungal effects. The goal of this review is to highlight recent developments in the synthesis and structure-activity relationship (SAR) investigation of this prospective fungicidal chemical. Also there have been explained drugs and mechanism of action of a triazole compound with antifungal activity. This review will be useful in a variety of fields, including medicinal chemistry, organic chemistry, mycology, and pharmacology.

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Saleem, Faiza, and Khalid Mohammed Khan. "Indole Derivatives: Unveiling New Frontiers in Medicinal and Synthetic Organic Chemistry." Molecules 28, no. 14 (July 18, 2023): 5477. http://dx.doi.org/10.3390/molecules28145477.

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In recent years, significant attention has been given to indoles, a diverse group of heterocyclic compounds widely found in nature that play a crucial role in various bioactive natural and synthetic substances [...]

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Jindal, Rani, and Sanjay Bajaj. "Recent Applications of Microwaves in Synthesis of Bioactive Heterocyclic Compounds." Current Organic Chemistry 12, no. 10 (July 1, 2008): 836–49. http://dx.doi.org/10.2174/138527208784911842.

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İ MAHMOOD, Israa, Salih SALMAN, and Luma ABD. "New Bioactive Aromatic Heterocyclic Macromolecules with Monosaccharide Core." Journal of the Turkish Chemical Society Section A: Chemistry 9, no. 3 (August 31, 2022): 889–900. http://dx.doi.org/10.18596/jotcsa.1098055.

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1,1,2-trimethyl-1H-benzo[e]indole is an important heterocyclic compound, its available in reasonable price and can easily modified to make a good intermediate for other derivatives. That is quite enough reasons to use as starting material for a new series of compounds with other biomolecules such as monosaccharides after simple modification. The target molecules show biological activity. So, the current work is aiming to improve the activity and the properties of the benzo indole by attaching with a naturally occurring, and biodegradable compounds represented by 2-deoxy-2-amino -d-glucose and 6-deoxy-6-amino-d-glucose to synthesis both mono and di-saccharides derivatives of benzo indole. Two steps synthesis were used for mono-saccharide derivatives and three steps for di-saccharide derivatives, the first is the functionalization of 1,1,2-trimethyl-1H-benzo[e]indole [1] via the reaction with POCl3 to produce 2-(1,1-dimethyl-1H-benzo[e]indol-2(3H)-ylidene) malonaldehyde [2] with two aldehydes reaction centers, while in the second step the latter was coupled with sugar via amino groups to get the two monosaccharide derivatives [3,5], while the disaccharides molecules [4,6] taken one more step with harder conditions to overcome the steric hindrance at the other reaction center. The purity and characterization of the target molecules was confirmed using spectroscopy methods including 1H NMR and 13 NMR. The synthesized compound shows a good biological activity as antibacterial antifungal.

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Thakral, Samridhi, and Vikramjeet Singh. "Recent Development on Importance of Heterocyclic Amides as Potential Bioactive Molecules: A Review." Current Bioactive Compounds 15, no. 3 (May 7, 2019): 316–36. http://dx.doi.org/10.2174/1573407214666180614121140.

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Background: Heterocyclic compounds are an integral part of the chemical and life sciences and constitute a considerable quantum of the modern research that is being currently pursued throughout the world. Methods: This review was prepared by collecting the available literature reports on various databases and an extract was prepared for each report after thorough study and compiling the recent literature reports on heterocyclic amides from 2007 to 2018. Results: This review summarizes the bio-potential of heterocyclic amides as antimicrobial, anticancer, anti-tubercular and antimalarial agents which would be very promising in the field of medicinal chemistry. Conclusion: A wide variety of heterocyclic amides have already been reported and some are currently being used as active medicaments for the treatment of disease. Still, the research groups are focusing on the development of newer heterocyclic amide derivatives with better efficacy, potency and lesser side effects. This area has got the tremendous potential to come up with new chemical entities of medicinal importance.

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Naqvi, Arshi. "Synthesis, Characterization and Drug-Likeness Predictions of 1,3-Thiazole and Benzothiazole Derivatives." Oriental Journal of Chemistry 34, no. 6 (December 4, 2018): 3134–39. http://dx.doi.org/10.13005/ojc/340660.

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Heterocyclic compounds bearing nitrogen and sulphur in the main skeleton are reported to be a bioactive group. Thiazole and benzothiazole moieties are biologically significant class of this group. This research focus on the synthesis and characterization of 1,3-thiazole and benzothiazole derivatives. Drug likeness predictions were also undertaken for these newly synthesized compounds.

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Ghahsare, Aref G., Zahra S. Nazifi, and Seyed M. R. Nazifi. "Structure-Bioactivity Relationship Study of Xanthene Derivatives: A Brief Review." Current Organic Synthesis 16, no. 8 (January 20, 2020): 1071–77. http://dx.doi.org/10.2174/1570179416666191017094908.

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: Over the last decades, several heterocyclic derivatives compounds have been synthesized or extracted from natural resources and have been tested for their pharmaceutical activities. Xanthene is one of these heterocyclic derivatives. These compounds consist of an oxygen-containing central heterocyclic structure with two more cyclic structures fused to the central cyclic compound. It has been shown that xanthane derivatives are bioactive compounds with diverse activities such as anti-bacterial, anti-fungal, anti-cancer, and anti-inflammatory as well as therapeutic effects on diabetes and Alzheimer. The anti-cancer activity of such compounds has been one of the main research fields in pharmaceutical chemistry. Due to this diverse biological activity, xanthene core derivatives are still an attractive research field for both academia and industry. This review addresses the current finding on the biological activities of xanthene derivatives and discussed in detail some aspects of their structure-activity relationship (SAR).

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AHMAD, NASEEM, MOHAMMAD IRFAN AZAD, ABDUL RAHMAN KHAN, and IQBAL AZAD. "BENZIMIDAZOLE AS A PROMISING ANTIVIRAL HETEROCYCLIC SCAFFOLD: A REVIEW." Journal of Science and Arts 21, no. 1 (March 30, 2021): 273–84. http://dx.doi.org/10.46939/j.sci.arts-21.1-b05.

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Heterocyclic derivatives are unavoidable in many fields of natural disciplines. These derivatives play numerous significant roles in research, medication, and nature. Nitrogenous heterocyclic derivatives extremely are the main target of concern in synthetic chemistry to ensue active natural products with pharmaceuticals and agrochemicals interest. Benzimidazole skeleton is another example of some active heterocyclic moiety that significantly contributes in the numerous bioactive of essential compounds. Benzimidazole skeleton is studied as a prominent moiety of biologically active compounds with various activities including antimicrobial, antiprotozoal, anticancer, antiviral, acetylcholinesterase, antihistaminic, anti-inflammatory, antimalarial, analgesic, anti-HIV and antitubercular. Therefore, in this review we summarize the various antiviral activities of several benzimidazole derivatives and outline the correlation among the structures of different benzimidazoles scaffold with their therapeutic significance.

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Manahil B Elamin, Amani Abd Elrazig Salman Abd Elaziz, and Emad Mohamed Abdallah. "Benzothiazole moieties and their derivatives as antimicrobial and antiviral agents: A mini-review." International Journal of Research in Pharmaceutical Sciences 11, no. 3 (July 8, 2020): 3309–15. http://dx.doi.org/10.26452/ijrps.v11i3.2459.

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Heterocyclic chemistry has provided an inexhaustible source of pharmaceutical molecules. Heterocyclic compounds such as benzothiazole moieties and its derivatives area substantial class of compounds in pharmaceutical chemistry and exhibited therapeutic capabilities, such as antitumor, anticancer, antioxidant, antidiabetic, antiviral, antimicrobial, antimalarial, anthelmintic and other activities. Besides, some antibiotics such as penicillin and cephalosporin have heterocyclic moiety. The growing prevalence of multi-drug resistant pathogens represents serious global concern,which requires the development of new antimicrobial drugs. Moreover, the emergence of pandemic SARSCoV-2 causing Covid-19 disease and all these health dilemmas urge the scientific community to examine the possible antimicrobial and antiviral capacities of some bioactive benzothiazole derivatives against these severe causative agents.This mini-review highlights some recent scientific literature on different benzothiazole molecules and their derivatives. It turns out that, there are numerous synthesized benzothiazole derivatives which exhibited different mode of actions against microorganisms or viruses and accordingly suggested them as an active candidate in the discovery of new antimicrobial or antiviral agents for clinical development. The recommended bioactive benzothiazole derivatives mentioned in the current study are mainly Schiff bases, azo dyes and metal complexes benzothiazole derivatives; the starting material for most of these derivatives are 2-aminobenzothiazole although careful pharmaceutical studies should be conducted to ensure the safety and efficacy of these bioactive synthesized molecules as an antimicrobial or antiviral drug in the future.

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Paz, Bruno Matos, Yang Li, Mathias Kirk Thøgersen, and Karl Anker Jørgensen. "Enantioselective synthesis of cyclopenta[b]benzofurans via an organocatalytic intramolecular double cyclization." Chemical Science 8, no. 12 (2017): 8086–93. http://dx.doi.org/10.1039/c7sc03006a.

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An enantioselective organocatalytic strategy, combining Brønsted base and N-heterocyclic carbene catalysis in a unique manner, is demonstrated for a concise construction of the privileged cyclopenta[b]benzofuran scaffold, present in many bioactive compounds having both academic and commercial interests.

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Rolava, Evija, Jevgeņija Lugiņina, and Māris Turks. "Glucose - and Allose-Derived Chiral Auxiliaries." Key Engineering Materials 800 (April 2019): 36–41. http://dx.doi.org/10.4028/www.scientific.net/kem.800.36.

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Oxazolidinones are an important class of heterocyclic compounds that are used as chiral auxiliaries in asymmetric synthesis and as biologically active pharmaceutical agents. Moreover, carbohydrates are ideal scaffolds to generate libraries of bioactive compounds due the presence of defined configuration. We report here asymmetric alkylation studies on N-derivatized glucose-and allose-based spirooxazolidinones which do act as chiral auxiliaries.

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Zhang, Xiaofeng, Miao Liu, Weiqi Qiu, and Wei Zhang. "2-Azidobenzaldehyde-Based [4+2] Annulation for the Synthesis of Quinoline Derivatives." Molecules 29, no. 6 (March 11, 2024): 1241. http://dx.doi.org/10.3390/molecules29061241.

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Quinoline is a privileged heterocyclic ring which can be found in many drug molecules and bioactive compounds. The development of synthetic methods for making quinoline derivatives continuously attracts the interest of organic and medicinal chemists. This paper highlights 2-azidobenzaldehyde-based [4+2] annulation for the synthesis of quinoline derivatives including fused and spiro-quinolines, quinoline-4-ols, 4-aminoquinolines, and related compounds.

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Ahmed A. El-Sayed, Nahid Y. Khaireldin, and Eman A. El-Hefny. "Review for metal and organocatalysis of heterocyclic C-H functionalization." World Journal of Advanced Research and Reviews 9, no. 1 (January 30, 2021): 001–30. http://dx.doi.org/10.30574/wjarr.2021.9.1.0071.

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Over the last few decades, signiﬁcant efforts have been put forth towards the C−H bond group functionalization by transition-metalcatalysis and organocatalysis. Several efficient strategies to convert C-H bond to other groups C-C, C-N, C-O bonds have been implemented. The most attractive C-H bond functionalization was the C-H heterocyclic compounds activation that is practical method in organic synthesis. The new C–C, C–N and C–O bond as formed from the C-H bond activation by two diverse ways metal catalysis and/or organocatalysis. The most important is the synthesis of new bioactive heterocyclic compounds by easy and less expensive materials. In this review, we will cover most of the syntheses of heterocyclic derivatives by the functionalization of C-H bond in metal and organocatalytic reagents.

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Athina, Geronikaki, Christophe Tratrat, Anthi Petrou, Maria Fesatidou, Michelyne Haroun, Katharigatta N. Venugopala, Nagaraja Sreeharsha, and Jad Chemali. "5-Membered Heterocyclic Compounds as Antiviral Agents." Current Topics in Medicinal Chemistry 23, no. 7 (March 2023): 520–38. http://dx.doi.org/10.2174/1568026623666230325153927.

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Abstract: Viral infections range from self-limiting to more serious and fatal infections; therefore, some viral infections are of great public health concern worldwide, e.g., Hepatitis B virus, Hepatitis C virus, and HIV. Recently, the world faced a new infection due to the coronavirus, COVID-19, which was announced as a pandemic in early 2020. This virus infected more than 500 million peo-ple, killing around 6 million people worldwide. On the other hand, the increase in drug-resistant strains is also creating serious health problems. Thus, developing new selective antiviral agents with a different mode of action to fight against mutated and novel viruses is a primary goal of many re-searchers. Taking into account the role of heterocyclic compounds in drug discovery as a key struc-tural component of most of the bioactive molecules; herein, we report an extensive review of the an-tiviral activity of five-membered heterocyclic compounds reported from 2015 to date. In this re-view, the antiviral activities of the agents containing the specified ring systems thiadiazoles, tria-zoles, oxadiazoles, and thiazoles are discussed.

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Abdallah, Magda A., Thoraya A. Farghaly, and Mohamed R. Abdel Aziza. "Exocyclic enaminones as building blocks for synthesis of bioactive polyheterocyclic compounds." JOURNAL OF ADVANCES IN CHEMISTRY 10, no. 6 (July 3, 2014): 2753–65. http://dx.doi.org/10.24297/jac.v10i6.880.

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The reaction of exocyclic enaminones namely, 2-(dimethylaminomethylene)-3,4-dihydro-2H-naphthalen-1-one, 3-(dimethylaminomethylene)-thiochroman-4-one and 2-(dimethyl-aminomethylene)-indane-1,3-dione, each with heterocyclic diazonium salts afforded the respective hydrazones which undergo either in situ dehydrative cyclization or cyclized by heating with acetic acid to give polycyclic compounds. The structure of all the newly synthesized products were confirmed by elemental and spectral (IR, IH NMR, Mass) data. Also, the biological activity of some of the prepared compounds was tested against some microorganisms and promising results were obtained.

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Pawlowski, Robert, Filip Stanek, and Maciej Stodulski. "Recent Advances on Metal-Free, Visible-Light- Induced Catalysis for Assembling Nitrogen- and Oxygen-Based Heterocyclic Scaffolds." Molecules 24, no. 8 (April 18, 2019): 1533. http://dx.doi.org/10.3390/molecules24081533.

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Heterocycles are important class of structures, which occupy a major space in the domain of natural and bioactive compounds. For this reason, development of new synthetic strategies for their controllable synthesis became of special interests. The development of novel photoredox systems with wide-range application in organic synthesis is particularly interesting. Organic dyes have been widely applied as photoredox catalysts in organic synthesis. Their low costs compared to the typical photocatalysts based on transition metals make them an excellent alternative. This review describes proceedings since 2015 in the area of application of metal-free, visible-light-mediated catalysis for assembling various heterocyclic scaffolds containing five- and six-membered rings bearing nitrogen and oxygen heteroatoms.

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Dawood, Kamal M., Thoraya A. Farghaly, and Mohamed A. Raslan. "Heteroannulation Routes to Bioactive Pyrazolooxazines." Current Organic Chemistry 24, no. 17 (November 12, 2020): 1943–75. http://dx.doi.org/10.2174/1570179417999200628035124.

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Pyrazolo-oxazine fused systems are interesting classes of heterocyclic compounds exhibiting pronounced biological applications such as anticancer, antitubercular, anti-inflammatory, antibacterial and antifungal activities as well as inhibiting COX-1 and COX-2 enzymes. Depending on the distribution position of the heteroatoms (N and O), there are fourteen different systems of pyrazolo-oxazine. Nine of them were biologically abundant in literature, for example, pyrazolo[3,4-e][1,3]oxazines are used as analogs of antibiotics Formycin, Formycin B, Oxoformycin B. This review article summarizes the concerted efforts expended on most of the synthetic routes to the various types of pyrazolo-oxazines in the literature until the first quarter of 2020. The reactions of pyrazolo-oxazines with various reagents are also outlined.

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34

Döndas, H., María de Gracia Retamosa, and José Sansano. "Current Trends towards the Synthesis of Bioactive Heterocycles and Natural Products Using 1,3-Dipolar Cycloadditions (1,3-DC) with Azomethine Ylides." Synthesis 49, no. 13 (June 7, 2017): 2819–51. http://dx.doi.org/10.1055/s-0036-1588423.

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This review summarizes the trends in the formation of complex or not so complex heterocyclic structures through 1,3-dipolar cycloadditions of azomethine ylides. Diastereo- and enantioselective processes as well as non-asymmetric cycloadditions constitute very important synthetic tools for achieving these compounds. This review covers the literature from 2015 through 2016 and organizes the research in terms of biologically important heterocycles and natural products from cascade 1,3-dipolar cycloadditions of azomethine ylides to the simpler forms of 1,3-dipolar cycloaddition.1 Introduction2 Synthesis of Spirooxindoles3 Synthesis of Spiropyrrolidines4 Synthesis of Spiropiperidines and Piperidines5 Synthesis of Pyrrolidines and Fused Pyrrolidines6 Synthesis of Pyrrolizidines and Indolizidines7 Synthesis of Quinolone and Isoquinolines8 Conclusions

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Rentería-Gómez, Manuel A., Luis E. Cárdenas Galindo, and Rocío Gámez-Montaño. "Synthesis of the 2-tetrazolylmethyl-2,3,4,9-tetrahydro-1H-β-carbolines via Ultrasound-Assisted One-Pot Ugi-azide/Pictet–Spengler Process." Proceedings 41, no. 1 (November 14, 2019): 67. http://dx.doi.org/10.3390/ecsoc-23-06515.

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A serie of 2-tetrazolylmethyl-2,3,4,9-tetrahydro-1H-β-carbolines were synthesized via a one pot Ugi-azide/Pictet–Spengler process under mild ultrasound-assisted conditions. The products containing two privileged heterocyclic frameworks: 1,5-disubstituted-1H-tetrazole and tetrahydro-β-carboline, which are present in a variety of bioactive compounds and commercial drugs.

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Majumdar, Krishna C., Pradip Debnath, Abu Taher, and Amarta K. Pal. "Intramolecular cyclization reaction — Palladium(0)-catalyzed cyclization is more effective than tin hydride mediated reaction." Canadian Journal of Chemistry 86, no. 4 (April 1, 2008): 325–32. http://dx.doi.org/10.1139/v08-023.

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Intramolecular CH arylation of pyrone, pyridone, uracil, imidazole, and benzimidazole derivatives are carried out in the presence of a Pd catalyst to form potentially bioactive fused heterocyclic compounds, whereas the n-Bu3SnH-mediated aryl radical cyclization of the precursors 3 afforded mainly halogen-reduced uncyclized products.Key words: Pd(0) catalyst, CH arylation, intramolecular cyclization, regioselectivity.

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Ardiansah, Bayu. "RECENT REPORTS ON PYRAZOLE-BASED BIOACTIVE COMPOUNDS AS CANDIDATE FOR ANTICANCER AGENTS." Asian Journal of Pharmaceutical and Clinical Research 10, no. 12 (December 1, 2017): 45. http://dx.doi.org/10.22159/ajpcr.2017.v10i12.22065.

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Pyrazole is a five-membered heterocyclic compound containing two nitrogen atoms. Due to its biological significance, design of novel pyrazole derivatives has become an interesting research area. We report the current progress in the development of anticancer agents containing pyrazole ring covering the time span of the past few years (2013–2016). The presence of this nucleus is accompanied with some side chains, functional groups, or in combination with other nucleus such as thiazole, thiourea, glucosamine, naphthalimide, and benzofuran. Several biologically active pyrazoles synthesized by numerous researchers across the world are summarized in this paper.

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Rentería-Gómez, Manuel A., and Rocío Gámez-Montaño. "Synthesis of 3-Tetrazolylmethyl-4H-Chromen-4-Ones Via Ugi-Azide Reaction Catalyzed by ZnO Nanoparticles." Proceedings 41, no. 1 (November 14, 2019): 69. http://dx.doi.org/10.3390/ecsoc-23-06517.

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A serie of novel 3-tetrazolylmethyl-4H-chromen-4-ones were synthesized via Ugi-azide reaction under mild ultrasound-assisted conditions (room temperature, EtOH, 10% mol ZnO nanoparticles). The products containing two privileged heterocyclic frameworks: 1,5- disubstituted-1H-tetrazole and 3-substituted-4H-chromen chromen-4-ones, which are present in a variety of bioactive compounds and commercial drugs

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Gomha, Sobhi M., Mastora M. Edress, Zeinab A. Muhammad, Hatem M. Gaber, Mohamed M. Amin, and Islam K. Matar. "Synthesis Under Microwave Irradiation and Molecular Docking of Some Novel Bioactive Thiadiazoles." Mini-Reviews in Medicinal Chemistry 19, no. 5 (February 21, 2019): 437–47. http://dx.doi.org/10.2174/1389557518666180329122317.

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Background: A novel series of fused imidazole was prepared from the reaction of 2- bromoacetyl-3-phenyl-1,3,4-thiadiazole with various heterocyclic amines under microwave irradiation. The structures of all the novel products were elucidated based on the elemental analysis and spectral data. </P><P> Results: In addition, the biological activity of the newly synthesized compounds was evaluated and the results obtained indicate their potency as anti-inflammatory, analgesic and anti- ulcer agents. </P><P> Conclusion: The binding mechanism of the most active compounds was studied using MOE to analyze the molecular interactions.

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Mahmoud, Huda, Magda Abdallah, and Thoraya Farghaly. "The Utility of Hydrazonoyl Halides in the Synthesis of Bioactive Heterocyclic Compounds." Current Organic Synthesis 14, no. 3 (March 1, 2017): 430–61. http://dx.doi.org/10.2174/1570179413666160624105624.

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Ghinea, Ioana Otilia, Andreea Veronica Dediu, Claudia Ungureanu, Bianca Furdui, Gabriela Bahrim, and Rodica Mihaela Dinica. "Measuring the cytotoxicity of bioactive N-heterocyclic compounds obtained via enzymatic catalysis." Journal of Biotechnology 208 (August 2015): S28—S29. http://dx.doi.org/10.1016/j.jbiotec.2015.06.076.

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Ferreira, Vitor F., Thais de B. da Silva, Fernanda P. Pauli, Patricia G. Ferreira, Luana da S. M. Forezi, Carolina G. de S. Lima, and Fernando de C. da Silva. "Dimroth´s Rearrangement as a Synthetic Strategy Towards New Heterocyclic Compounds." Current Organic Chemistry 24, no. 17 (November 12, 2020): 1999–2018. http://dx.doi.org/10.2174/1385272824999200805114837.

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Molecular rearrangements are important tools to increase the molecular diversity of new bioactive compounds, especially in the class of heterocycles. This review deals specifically with a very famous and widely applicable rearrangement known as the Dimroth Rearrangement. Although it has originally been observed for 1,2,3-triazoles, its amplitude was greatly expanded to other heterocycles, as well as from laboratory to large scale production of drugs and intermediates. The reactions that were discussed in this review were selected with the aim of demonstrating the windows that may be open by the Dimroth's rearrangement, especially in what regards the development of new synthetic approaches toward biologically active compounds.

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Abd-Ella, Aly A., Saoud A. Metwally, Mokhtar A. Abd ul-Malik, Yasser A. El-Ossaily, Fathy M. Abd Elrazek, Safwat A. Aref, Youssra A. Naffea, and Shaban A. A. Abdel-Raheem. "A review on recent advances for the synthesis of bioactive pyrazolinone and pyrazolidinedione derivatives." Current Chemistry Letters 11, no. 2 (2022): 157–72. http://dx.doi.org/10.5267/j.ccl.2022.2.004.

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Oxo derivatives of pyrazolines and pyrazolidines are important heterocyclic compounds due to their unique biological activities and have been widely applied in pharmaceutical and agromedical fields. In this review, we provide an account of some recent advances in the field of pyrazolone chemistry, specifically on the reported synthesis methods of pyrazolinone (3-oxo-1,2-dihydropyrazole) and 3,5-pyrzolidinediones (3,5-dioxotetrahydropyrazoles) derivatives.

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Khalaf, Zahraa D. "Synthesis, Spectral, Antioxidant and Antimicrobial Activity of Some New Heterocyclics containing Benzimidazole Moiety." Research Journal of Chemistry and Environment 26, no. 8 (July 25, 2022): 56–60. http://dx.doi.org/10.25303/2608rjce056060.

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Benzimidazole, as a model compound for the development of new bioactive compounds, has long been revered by organic and medicinal chemists due to unique properties of heterocyclic compounds. A comprehensive study of recent methods of synthesizing this compound will provide researchers, chemists and pharmacologists with the most up-to-date, most productive, cost-effective information possible. Benzimidazole compounds might be important in developing novel medications in the future because of their speedy, easy, efficient and environmentally friendly production, characterization and biological investigation. FTIR and 1HNMR data for the spectroscopic characterization; compared to BHT demonstrated significant antioxidant and antibacterial activity.

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Soares, José X., Daniela R. P. Loureiro, Ana Laura Dias, Salete Reis, Madalena M. M. Pinto, and Carlos M. M. Afonso. "Bioactive Marine Xanthones: A Review." Marine Drugs 20, no. 1 (January 8, 2022): 58. http://dx.doi.org/10.3390/md20010058.

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The marine environment is an important source of specialized metabolites with valuable biological activities. Xanthones are a relevant chemical class of specialized metabolites found in this environment due to their structural variety and their biological activities. In this work, a comprehensive literature review of marine xanthones reported up to now was performed. A large number of bioactive xanthone derivatives (169) were identified, and their structures, biological activities, and natural sources were described. To characterize the chemical space occupied by marine-derived xanthones, molecular descriptors were calculated. For the analysis of the molecular descriptors, the xanthone derivatives were grouped into five structural categories (simple, prenylated, O-heterocyclic, complex, and hydroxanthones) and six biological activities (antitumor, antibacterial, antidiabetic, antifungal, antiviral, and miscellaneous). Moreover, the natural product-likeness and the drug-likeness of marine xanthones were also assessed. Marine xanthone derivatives are rewarding bioactive compounds and constitute a promising starting point for the design of other novel bioactive molecules.

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Mariconda, Annaluisa, Marco Sirignano, Rubina Troiano, Simona Russo, and Pasquale Longo. "N-heterocyclic Carbene Gold Complexes Active in Hydroamination and Hydration of Alkynes." Catalysts 12, no. 8 (July 29, 2022): 836. http://dx.doi.org/10.3390/catal12080836.

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Until the year 2000, gold compounds were considered catalytically inert. Subsequently, it was found that they are able to promote the nucleophilic attack on unsaturated substrates by forming an Au–π-system. The main limitation in the use of these catalytic systems is the ease with which they decompose, which is avoided by stabilization with an ancillary ligand. N-heterocyclic carbenes (NHCs), having interesting s-donor capacities, are able to stabilize the gold complexes (Au (I/III) NHC), favoring the exploration of their catalytic activity. This review reports the state of the art (years 2007–2022) in the nucleophilic addition of amines (hydroamination) and water (hydration) to the terminal and internal alkynes catalyzed by N-heterocyclic carbene gold (I/III) complexes. These reactions are particularly interesting both because they are environmentally sustainable and because they lead to the production of important intermediates in the chemical and pharmaceutical industry. In fact, they have an atom economy of 100%, and lead to the formation of imines and enamines, as well as the formation of ketones and enols, all important scaffolds in the synthesis of bioactive molecules, drugs, heterocycles, polymers, and bulk and fine chemicals.

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Russo, Marina, Ivana Bonaccorsi, Germana Torre, Antonella Cotroneo, Paola Dugo, and Luigi Mondello. "Determination of Bioactive Compounds in the Juice of Pummelo (Citrus grandis Osbeck)." Natural Product Communications 8, no. 2 (February 2013): 1934578X1300800. http://dx.doi.org/10.1177/1934578x1300800209.

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The juice of pummelo (Citrus grandis Osbeck) was analyzed to determine its composition of flavonoids, polymethoxyflavones, coumarins and psoralens. The analyses were carried out by HPLC using columns packed with small diameter Fused-Core® C18 particles to achieve high resolution in short analysis time. In addition, the profile of the native carotenoids present in the juice was determined using a C30 column. Identification of flavonoids was achieved by MS with ESI in negative mode; the MS acquisition of oxygenated heterocyclic compounds was performed in positive APCI; carotenoids were detected with a PDA detector. Nineteen native carotenoids were determined in pummelo juice for the first time. The composition of this juice is also discussed in comparison with other Citrus juices, especially grapefruit.

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Contreras, J. Guillermo, and Sandra T. Madariaga. "Bioactive Four-Membered Heterocyclic Compounds: The Anti → Syn Interconversion in Dithietane-1,3-dioxide." Bioorganic Chemistry 29, no. 2 (April 2001): 57–64. http://dx.doi.org/10.1006/bioo.2000.1191.

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Champa, R., K. A. Vishnumurthy, Yadav D. Bodke, H. S. Bhojya Naik, Itte Pushpavathi, P. Meghana, and Priya R. Kadam. "Synthesis, characterization, and biological investigations of potentially bioactive heterocyclic compounds containing benzimidazole nucleus." Results in Chemistry 6 (December 2023): 101018. http://dx.doi.org/10.1016/j.rechem.2023.101018.

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Balandis, Benas, Vytautas Mickevičius, and Vilma Petrikaitė. "Exploration of Benzenesulfonamide-Bearing Imidazole Derivatives Activity in Triple-Negative Breast Cancer and Melanoma 2D and 3D Cell Cultures." Pharmaceuticals 14, no. 11 (November 13, 2021): 1158. http://dx.doi.org/10.3390/ph14111158.

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Heterocyclic compounds are one of the main groups of organic compounds possessing wide range of applications in various areas of science and their derivatives are present in many bioactive structures. They display a wide variety of biological activities. Recently, more and more attention has been focused to such heterocyclic compounds as azoles. In this work, we have synthesized a series of new imidazole derivatives incorporating a benzenesulfonamide moiety in their structure, which then were evaluated for their cytotoxicity against human triple-negative breast cancer MDA-MB-231 and human malignant melanoma IGR39 cell lines by MTT assay. Benzenesulfonamide-bearing imidazole derivatives containing 4-chloro and 3,4-dichlorosubstituents in benzene ring, and 2-ethylthio and 3-ethyl groups in imidazole ring have been determined as the most active compounds. Half-maximal effective concentration (EC50) of the most cytotoxic compound was 27.8 ± 2.8 µM against IGR39 cell line and 20.5 ± 3.6 µM against MDA-MB-231 cell line. Compounds reduced cell colony formation of both cell lines and inhibited the growth and viability of IGR39 cell spheroids more efficiently compared to triple-negative breast cancer spheroids.

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Journal articles on the topic 'Bioactive heterocyclic compounds'

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