Syntheses and Biological Activities of New Hybrid Molecules Containing Different Heterocyclic Moieties

Ceylan S., Bektas H., BAYRAK H., DEMİRBAŞ N., Alpay-Karaoglu S., Uelker S.

ARCHIV DER PHARMAZIE, vol.346, no.10, pp.743-756, 2013 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 346 Issue: 10
  • Publication Date: 2013
  • Doi Number: 10.1002/ardp.201300161
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.743-756
  • Keywords: Biological activity, Nicotinic acid hydrazide, 1, 3-Thia(oxa)zole, 1, 3-Thia(oxa)zolidinone, 1, 2, 4-Triazole, ANTIMICROBIAL ACTIVITY EVALUATION, UREASE ACTIVITY, DERIVATIVES, INHIBITORS, DESIGN, 1,2,4-TRIAZOLE, OBESITY, MANNICH
  • Karadeniz Technical University Affiliated: Yes


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.