Synthesis of Some Novel Thiazolidin-4-one Substituted 1, 2,4 - Triazoles of Their Antimicrobial Activity Studies

Thiazolidine-4-one substituted 1, 2, 4triazole and benzofuran heterocyclic have received considerable attention during last two decades as they are endowed with variety of biological activities and have wide range of therapeutic properties. A literature survey indicates that benzofuran derivatives possess different pharmacological and biological activities, of which the most potent is anti-microbial activity. When one biologically active molecule is linked to another, the resultant molecule generally has increased potency. Hence two pharmacophores, i.e. benzofuran and thiazolidine-4-one substituted 1,2,4-triazole are fused to obtain highly potent, more specific and less toxic antimicrobial agent The starting product 3-methoxybenzofuran hydrazide was prepared from methylsalicylate and diethylbromomalonate and hydrazine hydrate in three steps. The hydrazide was converted into the corresponding potassium dithiocabazinate, which on cyclization with hydrazine hydrate afforded 4-amino-3-(3-methoxy benzofuran)5-mercapto -1, 2, 4-triazoles. Condensation of triazoles with substituted aromatic benzaldehydes gave Schiff bases, which have been cyclized by treating with mercapto acetic acid. The compounds were characterized by elemental analysis and spectral data. All the compounds showed a very good antibacterial activity and significant the compounds VIIIe and VIIIf were found to possess broad-spectrum activity, while other compounds were found to exhibit moderate activities.