Novel 1,2,4-Triazolo[3,4-b]-1,3,4-thiadiazole Derivatives as Dual Analgesic/Anti-inflammatory and Antimicrobial Agents


TOZKOPARAN KÖPRÜCÜ B., Aytac S. P., Gursoy S., GÜNAL S., AKTAY G.

LETTERS IN DRUG DESIGN & DISCOVERY, vol.9, no.2, pp.204-212, 2012 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 9 Issue: 2
  • Publication Date: 2012
  • Doi Number: 10.2174/157018012799079626
  • Journal Name: LETTERS IN DRUG DESIGN & DISCOVERY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.204-212
  • Keywords: 4-Amino-3-mercapto-1,2,4-triazole, Analgesic activity, Anti-inflammatory activity, Antimicrobial activity, Antioxidant activity, 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole, MICHAEL ADDITION-PRODUCTS, ANTIINFLAMMATORY ACTIVITIES, PHARMACOLOGICAL-ACTIVITIES, HETEROCYCLIC SYSTEM, OXYGEN RADICALS, ACETIC-ACID, TRIAZOLOTHIADIAZOLES, IBUPROFEN, DRUGS, MOIETY
  • Inonu University Affiliated: Yes

Abstract

For this study, a series of 3,6-disubstituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles (1-12) were synthesized by condensation of 4-amino-5-substituted-3-mercapto-1,2,4-triazoles with various benzoic acids through a one-pot reaction. The anti-inflammatory and analgesic activities as well as gastrointestinal irritation liability of the obtained compounds were evaluated. Several of the synthesized compounds showed noticeable analgesic and anti-inflammatory activity. For the active compounds a very low ulcerogenic index and diminished oxidative damage in stomach were observed. Moreover, title compounds were screened for their antifungal and antibacterial activities. Antifungal activity of the compounds was found better than that of their antibacterial activity.