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

Birsen      Tozkoparan; Sevim      Peri Aytac; Sule      Gursoy; Selami      Gunal; Goknur      Aktay

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.

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, rheumatic diseases, nonsteroidal anti-inflammatory drugs (NSAIDs), gastrointestinal PUB (perforation,ulceration, and bleeding), ulcerogenic effect, co-administration, Thomas Hoover capillary melting point apparatus, FT-NMR instrument, DMSO-d6, CDCl3