Der Pharmacia Lettre

Abstract

Synthesis, characterization and biological evaluation of some novel condensed 3, 6-disubstituted-1,2,4-triazolo-1,3,4-thiadiazole derivatives

Author(s): P. Chaturvedi*, P. Valentina and P. Kamaria

In present study a new series of 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles derivatives(4a-j) were synthesized by hydrazinolysis of aromatic esters(methyl paraben and benzocaine) to give aryl hydrazides (1a-b), which were reacted with carbon disulphide and potassium hydroxide in ethanol to yield 3-substituted-5-mercapto- 1,3,4-oxadiazole(2a-b),which further cyclized to 4-amino-5-mercapto-1,2,4-triazoles(3a-b) by reacting with hydrazine hydrate. The resulted triazoles were converted to substituted triazolo-thiadiazoles (4a-j) by condensation with aromatic/hetro aromatic acids in presence of phosphorus oxychloride .The IR, 1H NMR and Mass spectral data were in accord with assigned structures. All the compounds were screened for antimicrobial, antifungal (Discdiffusion method and microdilution method) and Antioxidant activity (Hydrogen peroxide scavenging method). The result of pharmacological evaluation suggests that novel triazolo thiadiazole derivative of aromatic acids showed moderate antibacterial and antifungal activity while significant antioxidant activity as compared to standard drugs