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Journal articles on the topic 'Heterocyclic compounds – Synthesis'

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Published: 4 June 2021

Last updated: 29 January 2023

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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

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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3

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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4

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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5

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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6

Gupta, Vivek Kumar, Baljeet Kaur, Amandeep Kaur, Amanpreet Kaur, and Monika Gupta. "Synthesis and Biological Evaluation of 1,3,4-Oxadiazolyl benzenesulphonyl benzimidazole derivatives." Indian Journal of Pharmaceutical and Biological Research 6, no. 02 (June 30, 2018): 64–71. http://dx.doi.org/10.30750/ijpbr.6.2.10.

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Oxadiazoles are a class of heterocyclic aromatic chemical compound of azole family. Oxadiazole is five membered heterocycle having two carbons, two nitrogen, one oxygen and two double bonds. Oxadiazole exists in four isomeric forms depending upon the position of nitrogen atom in the ring. Benzimidazole is a heterocyclic aromatic compound. This bicyclic compound consists of fusion of benzene and imidazole. Benzimidazole may also be considered as cyclic analogues of imidines due to tautomerism effect. In the present study involves synthesis of1,3,4-oxadiazolyl benzenesulphonylbenzimidazole derivatives. All the synthesized compounds were screened against HepG-2 cell line to determine the growth inhibitory effect of compounds.All the synthesized compounds possessed good to moderate anti-cancer activity as compare to standard drug Adriamycin. Two of the synthesized compounds i.e. 8a and 8f were found to possess maximum anti-cancer activity.The structures of the synthesized compounds were established by IR and 1HNMR.

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7

Bakibayev, A. A., K. B. Zhumanov, S. Yu Panshina, S. I. Gorbin, V. S. Malkov, I. G. Tsoy, B. K. Massalimova, G. K. Matniyazova, and Е. А. Baybazarova. "Synthesis methods of phosphorylated carbamide containing acyclic and heterocyclic compounds." Bulletin of the Karaganda University. "Chemistry" series 95, no. 3 (September 30, 2019): 115–57. http://dx.doi.org/10.31489/2019ch3/115-157.

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8

Deng, Yongming, Qing-Qing Cheng, and Michael Doyle. "Asymmetric [3+3] Cycloaddition for Heterocycle Synthesis." Synlett 28, no. 14 (July 5, 2017): 1695–706. http://dx.doi.org/10.1055/s-0036-1588453.

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Asymmetric syntheses of six-membered ring heterocycles are important research targets not only in synthetic organic chemistry but also in pharmaceuticals. The [3+3]-cycloaddition methodology is a complementary strategy to [4+2] cycloaddition for the synthesis of heterocyclic compounds. Recent progress in [3+3]-cycloaddition processes provide powerful asymmetric methodologies for the construction of six-membered ring heterocycles with one to three heteroatoms in the ring. In this account, synthetic efforts during the past five years toward the synthesis of enantioenriched six-membered ring heterocycles through asymmetric [3+3] cycloaddition are reported. Asymmetric organocatalysis uses chiral amines, thioureas, phosphoric acids, or NHC catalysis to achieve high enantiocontrol. Transition-metal catalysts used as chiral Lewis acids to activate a dipolar species is an alternative approach. The most recent advance, chiral transition-metal-catalyzed reactions of enoldiazo compounds, has contributed toward the versatile and highly selective synthesis of six-membered heterocyclic compounds.1 Introduction2 Asymmetric Formal [3+3]-Cycloaddition Reactions by Organocatalysis2.1 By Amino-Catalysis2.2 By N-Heterocyclic Carbenes2.3 By Bifunctional Tertiary Amine-thioureas2.4 By Chiral Phosphoric Acids3 Asymmetric Formal [3+3]-Cycloaddition Reactions by Transition-Metal Catalysis3.1 Copper Catalysis3.2 Other Transition-Metal Catalysis4 Asymmetric [3+3]-Cycloaddition Reactions of Enoldiazo Compounds4.1 Asymmetric [3+3]-Cycloaddition Reactions of Nitrones with Electrophilic Metallo-enolcarbene Intermediates4.2 Dearomatization in Asymmetric [3+3]-Cycloaddition Reactions of Enoldiazoacetates4.3 Asymmetric Stepwise [3+3]-Cycloaddition Reaction of Enoldiazoacetates with Hydrazones5 Summary and Outlook

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9

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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10

Journal, Baghdad Science. "Synthesis of some Heterocyclic Compounds Derived from." Baghdad Science Journal 10, no. 3 (September 1, 2013): 525–36. http://dx.doi.org/10.21123/bsj.10.3.525-536.

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The 4-(?-bromo acetyl)-4?-toluene sulfonanilide (2) was used as key intermediate to synthesize new heterocyclic compounds. This bromo compound was synthesized via sulfonation of amino group of p-amino acetophenone using Hinsburg method with 4-toluene sulfonyl chloride to form 4-acetyl-4?-toluene sulfonanilide (1) which is used as a starting material in this work. This compound was brominated to yield compound (2) which is used as a precursor to synthesize new five and seven membered heterocyclic compounds such as substituted 1,3-oxazoles (3,4), 1,3-thiazole derivatives (5-7), thiourea compounds (8a,b), 1,3-Thiazoline-2-thione compounds (9a-f) and 1,2,5-triazepine compounds (11a-d). The synthesized compounds were identified depending upon physical, FT-IR and UV spectroscopic data.

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11

Zhu, Yannan, and You Huang. "Organocatalyzed [3+3] Annulations for the Construction of Heterocycles." Synthesis 52, no. 08 (February 5, 2020): 1181–202. http://dx.doi.org/10.1055/s-0039-1690810.

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Six-membered heterocyclic systems are widely distributed in many natural products and pharmaceuticals, and the construction of highly functionalized six-membered heterocyclic compounds is an important topic in modern organic synthesis. Organocatalyzed [3+3] annulations represents an important method for assembling a substantial variety of six-membered cycles that contain one or more heteroatoms. This review describes the development of organocatalyzed [3+3] annulations for the synthesis of six-membered heterocycles, including organocatalysis using secondary amines, tertiary amines, phosphines, chiral phosphoric acids and N-heterocyclic carbenes.1 Introduction2 Secondary Amine Catalyzed [3+3] Annulations2.1 Synthesis of Nitrogen Heterocycles2.2 Synthesis of Oxygen Heterocycles2.3 Synthesis of Sulfur Heterocycles3 Tertiary Amine Catalyzed [3+3] Annulations3.1 Catalysis through Multiple Hydrogen-Bonding Interactions3.2 Catalysis of Tertiary Amines as Lewis Bases4 Phosphine-Catalyzed [3+3] Annulations4.1 Synthesis of Nitrogen Heterocycles4.2 Synthesis of Oxygen Heterocycles4.3 Synthesis of Heterocycles Containing Two or More Heteroatoms5 Chiral Phosphoric Acid Catalyzed [3+3] Annulations5.1 Synthesis of Nitrogen Heterocycles5.2 Synthesis of Heterocycles Containing Two or More Heteroatoms6 N-Heterocyclic Carbene Catalyzed [3+3] Annulations6.1 Synthesis of Nitrogen Heterocycles6.2 Synthesis of Oxygen Heterocycles6.3 Synthesis of Heterocycles Containing Two or More Heteroatoms7 Conclusion and Outlook

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12

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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13

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 & regulatory assessment based on the ‘International Regulatory Standards’. Keywords: Heterocycles. Nitrogen containing compounds Biological activity, History, Regulatory assessment, International Regulatory Standards

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14

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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15

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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16

Biswas, Titas. "Synthesis of heterocyclic compounds using ring-closing enyne metathesis reaction." INTERNATIONAL JOURNAL OF EXPERIMENTAL RESEARCH AND REVIEW 22 (August 30, 2020): 20–29. http://dx.doi.org/10.52756/ijerr.2020.v22.003.

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Ring-closing enyne metathesis reaction has emerged as an elegant tool in organic synthesis for the creation of molecular complexity and used to prepare diverse heterocycles. In this mini review, I discuss that various linearly and angularly architecture heterocyclic compounds may be prepared using RCEM as key steps.

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17

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 & plan of recent remedial synthetic concoctions & 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 & hostile to microbial exercises. Furthermore, Heterocycles & medicines are both interred related, the human is totally dependent on drugs & most of the drugs are derived from heterocyclic compounds. Hetero cycles & their derivatives have been excited regards chemist mainly due to broad-spectrum chemical & pharmacological activities. Most of the heterocyclic compounds are naturally occurs & 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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18

Ranskiy, Anatoliy, Natalia Didenko, and Olga Gordienko. "Synthesis of Heterocyclic Thioamides and Copper(II) Coordination Compounds Based on Them." Chemistry & Chemical Technology 11, no. 1 (March 15, 2017): 11–18. http://dx.doi.org/10.23939/chcht11.01.011.

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19

Zouaoui, Emna, and Mohamed Moncef El Gaïed. "Synthesis of Trifluoromethyl Heterocyclic Compounds." Journal of Chemical Research 2003, no. 4 (April 2003): 242–46. http://dx.doi.org/10.1177/1747519803200300404.

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20

Sharad K. Awate, Suresh V. Patil, Ravindra S. Dhivare, and Renukacharya G. Khanapure. "Microwave-Assisted Synthesis, Characterization and Antimicrobial Potencies of N-Substituted Iminothiazodin-4-One Derivatives." International Journal of Research in Pharmaceutical Sciences 11, no. 1 (January 18, 2020): 589–95. http://dx.doi.org/10.26452/ijrps.v11i1.1861.

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The biggest and most multifaceted class of organic compounds includes heterocyclic compounds. Currently, several heterocyclic compounds are identified, and persistently gratefulness to tremendous synthetic work and synthetic usefulness, the number is increasing exponentially. In most fields of science, including medicinal, pharmaceutical, and agro-chemistry, heterocyclic compounds have a function, and biochemistry is also another area. In this research article, the green approach is administered for achieving the nitrogen, oxygen and sulphur centered five-membered heterocyclic derivatives. By taking the whole thing into account of hetero-chemistry, the moderately effective analog for gram-positive and gram-negative strains was shown for the five-membered heterocyclic compound series of N-substituted iminothiazodine-4-one and N-(benzylideneamino)thiazol-4(5H). The compound 6b showed very much active potency in accordance with the type standard drug the 6c compound against gram-positive Bacillus subtilis bacteria compared to the standard drugs and 6b indicated very active potency against the gram-negative Escherichia coli bacterial strain. The 5a and 6a compounds showed very strong activity against the fungal strain of Candida albicans and 6b or 6c were more active and highly potent than the standard drugs against Aspergillus niger species. In the view of this research, drive states that all the synthesized compounds might be used for the development for further heterocyclic entities.

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Manojkumar, Parameswaran, Thengungal Ravi, and Gopalakrishnan Subbuchettiar. "Synthesis of coumarin heterocyclic derivatives with antioxidant activity and in vitro cytotoxic activity against tumour cells." Acta Pharmaceutica 59, no. 2 (June 1, 2009): 159–70. http://dx.doi.org/10.2478/v10007-009-0018-7.

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Synthesis of coumarin heterocyclic derivatives with antioxidant activity andin vitrocytotoxic activity against tumour cellsThe aim of the present work was to synthesise coumarinyl heterocycles and to elucidate the potential role of these compounds as antioxidants and cytotoxic agents against Dalton's lymphoma ascites tumour cells (DLA) and Ehrlich ascites carcinoma cells (EAC). The synthesis of coumarin derivatives containing pyrazole, pyrazolone, thiazolidin-4-one, 5-carboxymethyl-4-thiazolidinone and 3-acetyl-1,3,4-oxadiazole ring is reported. 4-Methylcoumarinyl-7-oxyacetic acid hydrazide (1) reacted with arylazopropanes or hydrazono-3-oxobutyrate derivatives to form pyrazole (3a-c) and pyrazolone derivatives (5a-c). Heterocyclisation of Schiff's bases of 1 with thioglycolic acid, thiomalic acid or acetic anhydride afforded novel heterocyclic derivatives 4-thiazolidinones (7a-c), 5-carboxymethyl-4-thiazolidinones (8a-c) and oxadiazoles (9a-c), respectively. Some of the compounds showed promising antioxidant activityin vitroand cytotoxic activity against DLA cells and EAC cells.

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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

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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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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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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M, Vijey Aanandhi, Ravichandiran V, and Prem Shankar Misra. "SYNTHETIC ROUTES AND NATURAL SOURCES OF 2-PYRIDONE DERIVATIVES AND THEIR PHARMACOLOGICAL ACTIVITY." Asian Journal of Pharmaceutical and Clinical Research 10, no. 7 (July 1, 2017): 87. http://dx.doi.org/10.22159/ajpcr.2017.v10i7.17989.

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Objective: 2-pyridone is a well-known heterocyclic ring having significant biological and medical application. The molecular structures and various activities of 2-pyridone derivatives as well as their syntheses and natural occurrence are analyzed and reviewed, and their reactivity toward various nucleophiles is discussed.Methods: 2-pyridone derivatives, first naturally obtained and described as early as before the 19th century, have been attracting increasing attention in view of their high reactivity as building blocks for the preparation of compounds of various classes due to their selective transformations with different reagents. Much information describing the natural occurrence, synthesis and the significant biological activity of 2-pyridone compounds are scattered throughout the literature. There are short chapters dealing with the synthesis and activity of 2-pyridone derivatives.Results: After compiling the above material, the abundance of certain heterocyclic ring and nature of typical chemical transformations applied in current drug synthesis. It is likely this results from the abundance of these heterocycles in natural products such as alkaloids and various synthetic derivatives revealing different biological activity. This might suggest a classical approach to drug design where substrate analogs gain inspiration from existing natural ligands.Conclusions: The data considered in this review clearly demonstrate the high synthetic potential of 2-pyridone derivatives. Many biologically active heterocyclic compounds have been obtained based on this heterocyclic ring. This suggests that 2-pyridone can be used in the design of novel highly effective pharmaceuticals with a broad spectrum of bioresponses.

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Abdullah, Jasim Ali, and Muwafaq Ayesh Rabeaa. "Grinding-Assisted Synthesis of Some Heterocyclic Compounds." Asian Journal of Chemistry 32, no. 7 (2020): 1713–18. http://dx.doi.org/10.14233/ajchem.2020.22268.

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This article involves synthesis of some heterocyclic compounds from an amine derivative using ecofriendly approach (grinding). The first step involves synthesis of Schiff base from benzaldehyde derivatives (3-hydroxybenzaldehyde and 4-nitrobenzaldehyde) with 4-aminoantipyrine. These compounds were used as precursor for the synthesis of heterocyclic compounds and then synthesized tetrazole, oxazepine oxazepane derivatives from Schiff base with sodium azide, phthalic anhydride, maleic anhydride and succinic anhydride, respectively. The heterocyclic compounds were characterized by TLC, melting point, FTIR, 1H NMR, 13C NMR, GC-mass and HRMS analyses.

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Slivka, Mikhailo, and Mikhailo Onysko. "The Use of Electrophilic Cyclization for the Preparation of Condensed Heterocycles." Synthesis 53, no. 19 (May 19, 2021): 3497–512. http://dx.doi.org/10.1055/s-0040-1706036.

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AbstractCondensed heterocycles are well-known for their excellent biological effects and they are undeniably important compounds in organic chemistry. Electrophilic cyclization reactions are widely used for the synthesis of mono-heterocyclic compounds. This review highlights the utility of electrophilic cyclization reactions as an effective generic tool for the synthesis of various condensed heterocycles containing functional groups that are able to undergo further chemical transformations, such as nucleophilic substitution, elimination, re-cyclization, cleavage, etc. This review describes the reactions of unsaturated derivatives of different heterocycles with various electrophilic agents (halogens, arylsulfanyl chlorides, mineral acids) resulting in annulation of an additional partially saturated heterocycle. The electrophilic reaction conditions, plausible mechanisms and the use of such transformations in organic synthesis are also discussed. The review mainly focuses on research published since 2002 in order to establish the current state of the art in this area. 1 Introduction2 Electrophilic Cyclization Pathways Involving a Nitrogen Nucleophilic Center3 Electrophilic Cyclization Pathways Involving a Chalcogen Nucleophilic Center3.1 Sulfur Centers3.2 Oxygen Centers3.3 Selenium Centers4 Strategies and Mechanisms5 Conclusion

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Xu, Xinfang, and Michael P. Doyle. "Recent Developments in the Synthetic Uses of Silyl-protected Enoldiazoacetates for Heterocyclic Syntheses." Australian Journal of Chemistry 67, no. 3 (2014): 365. http://dx.doi.org/10.1071/ch13576.

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Diazo compounds have been used as precursors to a wide variety of heterocyclic compounds that represent the core structural subunits in many biologically active compounds. Various methodologies have been established for their synthesis via metal-catalyzed carbene transformations. Although the advantages of vinyldiazoacetates have been known for many years, realization of the synthetic use of enoldiazoacetates has been more recent. This review covers advances in the utility of silyl-protected enoldiazoacetates in heterocycle syntheses that include X–H insertion reactions, ylide rearrangements, formal [3+3]- and [4+3]-cycloaddition reactions, and other traditional and unusual metal carbene transformations.

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Bąchor, Urszula, and Marcin Mączyński. "Selected β2-, β3- and β2,3-Amino Acid Heterocyclic Derivatives and Their Biological Perspective." Molecules 26, no. 2 (January 15, 2021): 438. http://dx.doi.org/10.3390/molecules26020438.

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Heterocyclic moieties, especially five and six-membered rings containing nitrogen, oxygen or sulfur atoms, are broadly distributed in nature. Among them, synthetic and natural alike are pharmacologically active compounds and have always been at the forefront of attention due to their pharmacological properties. Heterocycles can be divided into different groups based on the presence of characteristic structural motifs. The presence of β-amino acid and heterocyclic core in one compound is very interesting; additionally, it very often plays a vital role in their biological activity. Usually, such compounds are not considered to be chemicals containing a β-amino acid motif; however, considering them as this class of compounds may open new routes of their preparation and application as new drug precursors or even drugs. The possibility of their application as nonproteinogenic amino acid residues in peptide or peptide derivatives synthesis to prepare a new class of compounds is also promising. This review highlights the actual state of knowledge about β-amino acid moiety-containing heterocycles presenting antiviral, anti-inflammatory, antibacterial compounds, anaplastic lymphoma kinase (ALK) inhibitors, as well as agonist and antagonists of the receptors.

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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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32

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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Ziarani, Ghodsi Mohammadi, Marzieh Rad, Fatemeh Mohajer, Hitesh Sehrawat, and Ravi Tomar. "Synthesis of Heterocyclic Compounds through Multicomponent Reactions Using 6-Aminouracil as Starting Reagent." Current Organic Chemistry 25, no. 9 (May 25, 2021): 1070–95. http://dx.doi.org/10.2174/1385272825666210303112858.

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The analogs of 6-Amino uracil are essential components due to their biological activities. The uracil is used as an important component for the synthesis of heterocyclic compounds like pyrrolo-, pyrido-, pyrimidine-pyrimido scaffolds. Herein, the application of this compound is reviewed as a precursor in the synthesis of many heterocyclic cores from 2016 to 2020.

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34

Zouaoui, Emna, and Mohamed Moncef El Gaïed. "Synthesis of trifluoromethyl heterocyclic compounds." Journal of Chemical Research 2003, no. 4 (April 1, 2003): 242–46. http://dx.doi.org/10.3184/030823403103173651.

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35

Ibrahim, Mohamed N., Mohamed F. El-Messmary, and Mohamed G. A. Elarfi. "Synthesis of Spiro Heterocyclic Compounds." E-Journal of Chemistry 7, no. 1 (2010): 55–58. http://dx.doi.org/10.1155/2010/604549.

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Reaction of isatin with acetophenone derivatives gave 3-hydroxy-3-phenacyl oxindole derivatives(II), dehydration of(II)gave 3-phenacylidene-2-indolinone derivatives(III). Condensation of(III)with hydrazine hydrate, phenylhydrazine and phenylthiourea afforded new spiropyrazolines(IV & V)and spiropyrimidinethione(VI)respectively. The structures of the final products were established by physical and spectral means.

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36

Al-awar, Rima, and George H. Wahl. "Microscale synthesis of heterocyclic compounds." Journal of Chemical Education 67, no. 3 (March 1990): 265. http://dx.doi.org/10.1021/ed067p265.

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37

Cullinane, N. M., and C. G. Davies. "Synthesis of some heterocyclic compounds." Recueil des Travaux Chimiques des Pays-Bas 55, no. 10 (September 3, 2010): 881–86. http://dx.doi.org/10.1002/recl.19360551009.

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38

Loughlin, Wendy A. "Invited Review. Combinatorial Synthesis: A Heterocyclic Chemist's Perspective." Australian Journal of Chemistry 51, no. 10 (1998): 875. http://dx.doi.org/10.1071/c98066.

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An overview of the combinatorial synthesis of heterocyclic compounds is presented. Recent developments and innovations in the solid and solution phase combinatorial synthesis of heterocyclic compounds are discussed.

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39

Parveen, Mehtab, Afroz Aslam, Shahab A. A. Nami, and Musheer Ahmad. "Z-Acrylonitrile Derivatives: Improved Synthesis, X-ray Structure, and Interaction with Human Serum Albumin." Current Organic Synthesis 16, no. 8 (January 20, 2020): 1149–60. http://dx.doi.org/10.2174/1570179416666191008085806.

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Aim and Objective: In the synthesis of heterocyclic compounds, acrylonitrile derivatives are the most important and appropriate precursors. These compounds are the most important intermediates and subunits for the enhancement of molecules having pharmaceutical or biological interests. Nitrogen-containing compounds have received extensive consideration in the literature over the years. Materials and Methods: A facile, economic and efficient method has been developed for the synthesis of acrylonitrile derivatives using p-nitrophenylacetonitrile and aromatic/heterocyclic aldehydes in the presence of zinc chloride at room temperature. Spectroscopic data were obtained using the following instruments: Fourier transform infrared spectra (KBr discs, 4000-400 cm-1) by Shimadzu IR-408 Perkin-Elmer 1800 instrument; 1H NMR and 13C NMR spectra by Bruker Avance-II 400 MHz using DMSO-d6 as a solvent containing TMS as the internal standard. Results: To continue our ongoing studies to synthesize heterocyclic and pharmaceutical compounds by mild, facile and efficient protocols, herein we wish to report our experimental results on the synthesis of acrylonitrile derivatives, using various aromatic/heterocyclic aldehydes and p-nitrophenylacetonitrile in the presence of zinc chloride in ethanolic media at room temperature. Some of the new compounds were tested for their human serum albumin activity (HSA) while a study of interaction with HSA protein was performed for compounds 3a and 3b. The results show that compound 3b binds tightly to HSA as compared to compound 3a. Conclusion: It can be concluded that acrylonitrile derivatives can be synthesized by an efficient method via the reaction of p-nitrophenylacetonitrile with aromatic/heterocyclic aldehydes by the use of zinc chloride as an effective solid catalyst. The remarkable features of this procedure include excellent yields (90-95%), short reaction period (30 min.), moderate reaction environment, easy workup procedure and managing of the catalyst. This method may find a wide significance in organic synthesis for the synthesis of the Z-acrylonitrile.

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40

Haji, Mohammad. "Multicomponent reactions: A simple and efficient route to heterocyclic phosphonates." Beilstein Journal of Organic Chemistry 12 (June 21, 2016): 1269–301. http://dx.doi.org/10.3762/bjoc.12.121.

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Multicomponent reactions (MCRs) are one of the most important processes for the preparation of highly functionalized organic compounds in modern synthetic chemistry. As shown in this review, they play an important role in organophosphorus chemistry where phosphorus reagents are used as substrates for the synthesis of a wide range of phosphorylated heterocycles. In this article, an overview about multicomponent reactions used for the synthesis of heterocyclic compounds bearing a phosphonate group on the ring is given.

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Cano, Jessica R. Gutiérrez, Julio López, Miguel A. Vázquez, David Cruz Cruz, and Clarisa Villegas Gómez. "Trienamines for the Organocatalytic Synthesis of Nitrogen-Containing Heterocycles." Current Organic Chemistry 23, no. 10 (August 16, 2019): 1078–89. http://dx.doi.org/10.2174/1385272823666190617164651.

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Nitrogen-containing heterocycles (NCH), constitute an important group of molecules, which are widely extended in whole chemical space. These compounds are of great interest due to their diverse biological activities. Currently, many compounds derived from NCH are used as powerful drugs for the treatment of diseases ranging from bactericides to anticancer agents. During last decade, the enantioselective synthesis of numerous heterocyclic compounds has been achieved through the use of chiral organocatalysts. The present contribution explores the application of the aminocatalysis towards the synthesis of NCH, particularly through the trienamine catalysis.

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42

BALUJA, S., D. MENPARA, S. CHANDA, and K. NANDHA. "SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME NEW PYRAZOLO QUINAZOLINE DERIVATIVES." Latin American Applied Research - An international journal 45, no. 3 (July 31, 2015): 157–63. http://dx.doi.org/10.52292/j.laar.2015.391.

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Pyrazolo[5,1-b]quinazolines are known to be versatile heterocyclic compounds with different biological properties because of a large number of derivatives with different structural modifications. Therefore, some new Pyrazolo quinazoline heterocycles were synthesized from chalcones and their structures were confirmed by IR, 1H NMR, 13C NMR and Mass spectral data. All these synthesized compounds were tested in vitro for their antimicrobial potential against Gram positive, Gram negative strains of bacteria as well as fungal strains in dimethylsulfoxide. Among the screened compounds, KC-10 showed the most potent antimicrobial activity. None of the compound shows antifungal activity. This may be due to the fact that fungal cells are complex organisms as compared to bacterial cell. Furthermore, the presence of S-CH3 group in the synthesized compounds may cause inactive behavior of these compounds against the studied fungal strains.

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Philkhana, Satish Chandra, Fatimat O. Badmus, Isaac C. Dos Reis, and Rendy Kartika. "Recent Advancements in Pyrrole Synthesis." Synthesis 53, no. 09 (March 17, 2021): 1531–55. http://dx.doi.org/10.1055/s-0040-1706713.

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AbstractThis review article features selected examples on the synthesis of functionalized pyrroles that were reported between 2014 and 2019. Pyrrole is an important nitrogen-containing aromatic heterocycle that can be found in numerous compounds of biological and material significance. Given its vast importance, pyrrole continues to be an attractive target for the development of new synthetic reactions. The contents of this article are organized by the starting materials, which can be broadly classified into four different types: substrates bearing π-systems, substrates bearing carbonyl and other polar groups, and substrates bearing heterocyclic motifs. Brief discussions on plausible reaction mechanisms for most transformations are also presented.1 Introduction2 From π-Systems2.1 Alkenes2.2 1,6-Dienes2.3 Allenes2.4 Alkynes2.5 Propargylic Groups2.6 Homopropargylic Amines3 From Carbonyl Compounds3.1 Aldehydes3.2 Ketones3.3 Cyanides and Isocyanides3.4 Formamides3.5 β-Enamines3.6 Dicarbonyl Compounds4 From Polar Compounds4.1 Aminols4.2 Diols4.3 Organonitro Compounds5 From Heterocycles5.1 Münchnones5.2 Isoxazoles5.3 Carbohydrates5.4 trans-4-Hydroxy-l-prolines5.5 Pyrrolines6 Summary

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Giubellina, Nicola, Wim Aelterman, and Norbert De Kimpe. "Use of 3-halo-1-azaallylic anions in heterocyclic chemistry." Pure and Applied Chemistry 75, no. 10 (January 1, 2003): 1433–42. http://dx.doi.org/10.1351/pac200375101433.

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The synthetic potential of lithio 3-halo-1-azaallylic anions as building blocks in organic chemistry and especially in heterocyclic chemistry will be highlighted by the synthesis of functionalized imines, obtained after reaction of 3-halo-1-azaallylic anions with het- eroatom-substituted electrophiles. Thus, the latter generated functionalized imines are suitable building blocks for the synthesis of a whole range of heterocycles and physiologically active compounds, including agrochemicals and pharmaceuticals. 3-Halo-1-azaallylic anions were used in the synthesis of N-alkyl-3,3-dichloroazetidines, 2,3-disubstituted pyrroles, piperidines, 2-substituted pyridines, 2-alkoxytetrahydrofurans,etc., from which a large range of useful and interesting chemicals can be produced, e.g., 2-azetines and 9-alkyl- 2-phenyl-3a-beta,4,6,7,8,9,9a-beta,9b-beta-octahydro-1H-pyrrolo [3,4,h]quinoline-1,3-diones. The utility of the present methodology is demonstrated by the synthesis of the pheromone (S)-manicone, the sulfur-containing flavor compound 2-[(methylthio)methyl ]-2-butenal, and some agrochemical and pharmaceutical compounds.

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45

Sharma, Kirti, Sumesh Chandra Sharma, and Mohit Kapoor. "Synthesis of Heterocyclic Compounds Via 1,3-Diketones." ECS Transactions 107, no. 1 (April 24, 2022): 9747–61. http://dx.doi.org/10.1149/10701.9747ecst.

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Heterocyclic compounds acquire a unique place in medicinal chemistry as many of the pharmaceuticals, agrochemical industries use heterocyclic moieties in different kinds of drugs. Moreover, many of these compounds are naturally occurring and are known for their antibacterial properties from ancient times. These compounds like thiazole, pyrazole, imidazole, coumarin etc. are synthesized via 1,3-dicarbonyls as an intermediate. Essentially β-dicarbonyls are considered as promising scaffolds for the synthesis of heterocyclic compounds. Especially, due to keto-enol tautomerism, β-diketones show very distinct chemical properties. They could be made by combining an adequate methyl ketone with an acceptable ethyl ester in a Claisen reaction, which allows for a large range of potential combinations. In this review, we will discuss various synthetic approaches for the preparation of five and six membered heterocyclic compounds via 1,3-dicarbonyls.

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Perlmutter, Patrick. "The Nucleophilic Addition/Eiectrophilic Ring Closure Route to Bio-Active Heterocycles." Current Medicinal Chemistry 3, no. 2 (April 1996): 139–52. http://dx.doi.org/10.2174/092986730302220302101738.

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Abstract: Many bio-active compounds contain one or more saturated or partially saturated heterocycles. Most of these contain one or more stereo centres. As a result any attempts to synthesize these compounds must take full account of the stereochemistry. In this article a new approach to the stereoselective synthesis of heterocycles is reviewed. The emphasis is on oxygen-containing heterocycles. The approach involves a sequence of a nucleophilic addition reaction followed by an electrophilic ring closure. Examples are given of the stereoselective synthesis of the heterocyclic subunits of macrolide and polyether antibiotics, ybutyrolactone autoregulators, marine polyether toxins and C-glycosides.

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Sbei, Najoua, Anna V. Listratova, Alexander A. Titov, and Leonid G. Voskressensky. "Recent Advances in Electrochemistry for the Synthesis of N-Heterocycles." Synthesis 51, no. 12 (May 7, 2019): 2455–73. http://dx.doi.org/10.1055/s-0037-1611797.

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The construction of N-heterocyclic rings represents a very important and fast-developing area of organic synthesis. In this context, electrochemistry has emerged as a mild solution for generating in situ the required electrophilic substrates, bases and nucleophiles derived from low-level and extremely stable reagents, the further application of which makes some heterocycles more accessible. In this review, we have covered the recent advances in the electrochemical synthesis of five- and six-membered N-heterocyclic compounds published from 2017 to October 2018.1 Introduction2 Electrochemical Synthesis of Five-Membered N-Containing Heterocycles2.1 Pyrrolidines2.2 Imidazoles2.3 Pyrazoles2.4 Triazoles2.5 Oxazoles2.6 Indoles2.7 Thiazoless3 Electrochemical Synthesis of Six-Membered N-Containing Heterocycles3.1 Piperidines and Pyridines3.2 Quinazolinones3.3 Benzoxazines4 Conclusions

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S. Farhan, Mohammed, and Kawkab Y. Saour. "Synthesis of some Novel Nitrogenous Heterocyclic Compounds with Expected Biological Activity as Antimicrobial and Cytotoxic Agents." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN 1683 - 3597 E-ISSN 2521 - 3512) 24, no. 1 (March 27, 2017): 49–58. http://dx.doi.org/10.31351/vol24iss1pp49-58.

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This study includes synthesis of some nitrogenous heterocyclic compounds linked to amino acid esters or heterocyclic amines that may have a potential activity as antimicrobial and/or cytotoxic. Quinolines are an important group of organic compounds that possess useful biological activity as antibacterial, antifungal and antitumor .8-Hydroxyquinoline (8-HQ) and numerous of its derivatives exhibit potent activities against fungi and bacteria which make them good candidates for the treatment of many parasitic and microbial infection diseases. These pharmacological properties of quinolones aroused our interest in synthesizing several new compounds featuring heterocyclic rings of the quinoline derivatives linked to amino acid ester or heterocyclic amine with the aim of obtaining a pharmacologically active compounds.O-alkylation has been done on( 8-hydroxyquinoline ) to get (O-alkylated ester) derivatives which are deesterfied to get acetic acid derivatives, then coupled with amino acid that have protected carboxyl group (amino acid esters) or heterocyclic amine by using conventional solution method for peptide synthesis as a coupling method. The proposed analogues were successfully synthesized and the processing of the reactions confirmed by TLC ,the synthesized analogues with the proposed structures as they were characterized and proved by melting point, infrared spectroscopy (IR) and elemental microanalysis. The tested analogues showed cytotoxic activity on the HEp-2 cell line (tumor of larynx) with inhibitory concentration percent of (IC %) range (32.43 % - 49.55%) and showed that the tested compounds had variable antimicrobial activities against selected bacteria and yeast when compared with selected standard drugs. Keywords: Quinolones, 8-hydroxyquinoline , N-heterocycles biological activity.

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Gupta, Monika. "Synthesis and Anti Proliferative Activity of Thiosemicarbazone and 4-Thiazolidinones." International Journal of Pharmacognosy & Chinese Medicine 3, no. 3 (2019): 1–9. http://dx.doi.org/10.23880/ipcm-16000166.

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Thiosemicarbazone and 4-Thiazolidinones are heterocyclic compounds with a broad spectrum of biological activities such as anti-inflammatory, anti-viral, anti-bacterial, anti-fungal and anticancer. A series of ten derivatives of thiosemicarbazone and 4-thiazolidinones derivatives was synthesised and evaluated for their antiproliferative activity against human breast cancer cells (MCF-7). The structure of compounds was established by IR and 1HNMR spectral studies. The synthesized compounds possessed good to moderate anticancer activity using Adriamycin as a standard. Out of ten synthesized compounds eight have GI50 value of <10 µg/ml demonstrating their potential activity. TGI for compound 6d was found to be comparable to Adriamycin (<10 µg/ml).

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50

Kottakki, Naveen K., and Amperayani K. Rao. "SYNTHESIS OF PIPERINE - PIPERAZINE ANALOGUES AND THEIR ANTIBACTERIAL ACTIVITY." INDIAN DRUGS 58, no. 06 (August 17, 2021): 30–35. http://dx.doi.org/10.53879/id.58.06.12311.

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In the current study, a series of piperine – piperazine analogues (5a to 5f) were designed and synthesized. The piperine was isolated from pepper and used for the conjugation with heterocyclic moiety for better biological activity. The piperazine heterocyclic was chosen for conjugation with piperine. The newly synthesized structures were determined by IR, 1H NMR and 13C NMR spectral data. The compounds were examined for their anti‐microbial activity against gram-positive (Bacillus subtilis) and gram-negative (Vibrio cholerae) bacteria using the agar well diffusion method. The newly synthesized compounds exhibited capable activities against V. cholerae and B. subtilis and it showed minimum inhibitory concentration. Among all the synthesized compounds, 5f has the highest activity (26 mm) against gram-positive bacteria and (29mm) against gram-negative bacteria. The remaining compounds showed appreciable antibacterial activity. The enhanced activity of the synthesized compounds may be due to the presence of conjugated amide linkage with the natural product piperine and piperazine heterocyclic molecule. The substituents present on the aromatic (nitro-substituted) ring also influenced the activity of the compound.

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