DESIGN AND SYNTHESIS OF SOME NEW 1,2,4-TRIAZOLE DERIVATIVES AS POTENTIAL ANTIBACTERIAL AGENTS

作者：Hayallah Alaa M^*; Sayed Ibrahim M

来源：Bulletin of Pharmaceutical Sciences, 2013, 36: 117-128.

Triazoles with different substituent groups are found to possess diverse applications in the field of medicinal chemistry. A new series of novel 1,3,5-trisubstituted[1,2,4]triazole derivatives, their Schiff bases and their amide derivatives were synthesized. Schiff bases (6-10) were prepared by the reaction of the triazoles amine 5 with equimolar amounts of the appropriate substituted benzaldehydes. The amide derivatives (25-39) were obtained by condensation of triazole amines (21-24) with the appropriate acid chloride. Chemical structures were confirmed by IR, H-1-NMR, C-13-NMR, FAB-MS, EI-HRMS spectra and elemental analyses. All the newly synthesized compounds were tested for in vitro activity against certain strains of bacteria such as Staph. aureus, Staph. saprophyticus, Escherichia coli and Bacillus cereus. Most of the tested new compounds exhibited promissing antibacterial activity. Some of them showed antibacterial activity more significant than the reference drugs. Compounds 6-10, 33, 36 and 39 were the most potent derivatives.

• 出版日期2013