Studies on Synthesis and Pharmacological Activities of 1,2,4‐Triazolo[3,4‐b]1,3,4‐thiadiazoles and their Dihydro Analogues

Abstract

4-Amino-5-substituted aryl-3-mercapto-1,2,4-triazoles are versatile synthons for constructing various biologically active heterocycles. Starting from 4-amino-5-substituted aryl-3-mercapto-1,2,4-triazole 3a-c, a series of new 3,5-disubstituted-1,2,4-triazolo-[3,4-b]1,3,4-thiadiazoles and their 5,6-dihydrotriazolothiadiazoles were prepared. The structures of all the newly synthesized compounds have been confirmed by elemental analysis, IR,( 1)H-NMR, (13)C-NMR, and mass spectra. The antimicrobial effects of the synthesized compounds were investigated using the paper disc method. Anti-inflammatory and analgesic activities of the synthesized compounds were assessed by carrageenan-induced rat paw oedema method and by Eddy's hot plate method, respectively. Some of the compounds exhibited promising antimicrobial activities as well as moderate to good anti-inflammatory activity and analgesic activity.

Synthesis, characterization and antimicrobial screening of thiazole based 1,3,4-oxadiazoles heterocycles

“…Thiazole derivatives have been reported to possess significant and diverse biological activities such as antimicrobial [3], analgesic [4], anti-inflammatory [5], antioxidant [6], anti HIV [7] and antitubercular [8,9] activities. Moreover, thiazoles are also synthetic intermediates and substructures in several biologically active compounds [10][11][12][13][14][15][16].…”

Synthesis of substituted 1, 2, 4-triazole derivatives by Microwave irradiation

“…The biological activity of 1,2,4-triazoles and their derivatives have been demonstrated by various studies 1,2. For instance, data came from previous investigations showed that 1,2,4-triazole nucleus posses a wide range of pharmacological activities such as analgesic 3 , antibacterial 4 , antifungal 5 ,anti-inflammatory 6 Microwave assisted organic synthesis 7 became an increasingly popular technique in academic and industrial research laboratories, due to certain advantages, particularly shorter reaction times and rapid optimization of chemical reactions. The experimental technique applied for the organic syntheses described below, is based on microwave power processing of materials using a dynamic control of the microwave power magnetron.…”

Studies on fused heterocyclic 3,6-disubstituted-1,2,4-triazolo-1,3,4-thiadiazoles: synthesis and biological evaluation

“…In addition to these important biological applications, mercapto-1,2,4-triazoles are also of great utility in preparative/synthetic organic chemistry, for example, in the presence of various reagents, undergo different types of reactions to yield other heterocyclic compounds, e.g., thiazolotriazoles, triazolothiadiazoles, triazolothiazines, triazolothiazepines, and triazolothiadiazines. Derivatives of 1,2,4-triazole and 1,3,4-thiadiazole condensed nucleus systems (triazolothiadiazoles) found to have diverse pharmacological activities including unique anti-inflammatory, anti-edema, and analgesic properties (Mathew et al, 2006(Mathew et al, , 2009Karthikeyan et al, 2007;Karegoudar et al, 2008;Prasad et al, 2009). Several triazolothiadiazole derivatives have been prepared from different non-steroidal anti-inflammatory agents and found to possess improved pharmacological profile (Udupi et al, 2004;Metwally et al, 2007;Amir et al, 2007).…”