6-benzylidenethiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones substituted with ibuprofen: synthesis, characterization and evaluation of anti-inflammatory activity


Tozkoparan B., Gokhan N., AKTAY G., Yesilada E., Ertan M.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol.35, pp.743-750, 2000 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 35
  • Publication Date: 2000
  • Doi Number: 10.1016/s0223-5234(00)00157-4
  • Title of Journal : EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
  • Page Numbers: pp.743-750
  • Keywords: 3-[1-(4-(2-methylpropyl)phenyl)ethyl]-1,2,4-triazole-5-thione, 6-benzylidenethiazalo[3,2-b]-1,2,4-triazole-5(6H)-ones, synthesis, anti-inflammatory activity, BRIDGEHEAD NITROGEN-HETEROCYCLES, ANTIINFLAMMATORY AGENTS, BIOLOGICAL-ACTIVITY, DERIVATIVES, ACIDS

Abstract

In this study, the synthesis of 3-[1-(4-(2-methylpropyl)phenyl)ethyl]-1,2,4-triazole-5-thione (2) and its condensed derivatives 6-benzylidenethiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones (2a-u) are described. The structures of the compounds were elucidated by spectral and elemental analysis. In the pharmacological studies, anti-inflammatory activities of these compounds have been screened. Among the compounds examined, the compounds 2 and 2g possessed the most prominent and consistent activity. In gastric ulceration studies the synthesized compounds were generally found to be safe at a 200 mg/kg dose level. (C) 2000 Editions scientifiques et medicales Elsevier SAS.