Synthesis of some 4-Amino-5-(substituted-phenyl)-4H-[1, 2, 4] triazole-3-thiol derivatives and Antifungal activity

Abstract

Despite the remarkable progress in diagnostic and antifungal drugs research in past 10 years ,still complexity of the characteristics of patients continue to make the management of fungal infection is a great challenge .1,2,4-triazole compounds not only offer an interesting chemistry but also their various derivatives possesses diverse chemotherapeutic activity. The recent literatures are enriched with the progressive finding about the synthesis and biological activity of 1,2,4-triazole heterocyclic compounds .4 amino -1,2,4-triazole -3-thiol are known to exhibit diverse pharmacological profile including analgesic anti-inflammatory  ,anti allergic ,anti viral ,anti–hiv, anti microbial ,anticonvulsant ,anti depressant ,antifungal, anti cancerous ,anti bacterial and anti tubercular activities. A series of 4 amino -5-(substituted phenyl-4H[1,2,4]-triazole -3-thiol were synthesized by cyclization of thiocarbohydrazide  and substituted benzoic acid by fusing method.4-(4-substitutedbenzylideneamino)-5(substitutedphenyl)-2H-1,2,4-triazole-4(4H)thione was prepared by condensation of primary amine of 4-Amino-5-(substituted phenyl)- 4H[1,2,4]-triazole -3-thiol with various substituted aromatic aldehyde through a single step and 4-(4- substituted benzylideneamino)-2-(morpholinomethyl). 5(substituted phenyl)-2H-1,2,4-triazole-4(4H)thione were afforded by the reaction of corresponding Schiff base with formaldehyde and morpholine with the formation of Iminium ion. Elemental analysis, IR,1H NMR & MASS spectral data confirmed the structure of newly synthesized compounds .Synthesized triazole investigated for antifungal activity .some of tested compounds show good and moderate antifungal activity against various antifungal strains.