Syntheses and biological activities of new hybrid molecules containing different heterocyclic moieties
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2013Author
Ceylan, ŞuleBektaş, Hakan
Bayrak, Hacer
Demirbaş, Neslihan
Karaoğlu, Şengül Alpay
Ülker, Serdar
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Ceylan, S., Bektas, H., Bayrak, H., Demirbas, N., Alpay-Karaoglu, S., & Ulker, S. (2013). Syntheses and biological activities of new hybrid molecules containing different heterocyclic moieties. Archiv der Pharmazie, 346(10), 743–756. https://doi.org/10.1002/ardp.201300161Abstract
4-Aryl-5-(pyridin-3-yl)-4H-1,2,4-triazole-3-(thi)oles 5-7, obtained starting from nicotinic acid hydrazide were converted to the corresponding Mannich bases 12-24 by the reaction with several heterocyclic amines in the presence of formaldehyde. The synthesis of S-alkylated compounds 8-11 was performed from the reaction of the corresponding triazol-5-thioles with various alkyl halides. The condensation of carbo(thio)amides 2-4 with 4-chlorophenacyl bromide afforded the corresponding 1,3-thia(oxa)zol-2(3H)-ylidene]pyridine-3- carbohydrazides 25-27. 1,3-Thia(oxa)zolidine derivatives 28-30 were obtained from the cyclization reaction between compounds 2-4 and ethyl bromoacetate. All newly synthesized compounds were screened for their antimicrobial, antiurease, and antilipase activities. The biological activity studies revealed that all the compounds screened showed good or moderate antimicrobial, antiurease, and/or antilipase activity. © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.