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

Document Type : Original Article

Authors

1 Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt

2 Department of Medical Microbiology and Immunology, Faculty of Medicine, Assiut University, Assiut 71526, Egypt

Abstract

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, 1H-NMR, 13C-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.