Synthesis, Characterization and Antibacterial Evaluation of Some Azole Derivatives

Abstract

Purpose: Tremendous rise in development of resistance to the antimicrobials has created alarming situation for researchers and clinicians.Method: In this regard, an attempt has been made to develop a series of azole derivatives using Claisen-Schmidt condensation and Micheal addition. All the newly synthesized compounds were authenticated by IR, 1H NMR, 13C NMR and MS spectral analysis. Synthesized compounds 5 (a-e) and 6 (a-e) were screened for their antibacterial activity against three Gram positive bacteria (S. aureus, B. subtilis and B. cereus), two Gram negative bacteria (E. coli and P. fluorescens) using serial dilution broth method.Results: Amongst all, Compound 5-(4-Chlorophenyl)-4-(3, 5-dimethyl-1H-pyrazol-1-yl)-3-phenylisoxazole (5 b) showed significant antibacterial activity against B. subtilis and B. cereus (IC50; 2.6 and 1.2 μg/mL) which was comparable to standard ampicillin (2.5 and 3.1 μg/mL).Conclusion: Azole derivatives were prepared using Claisen-Schmidt condensation and Micheal addition exhibits good antibacterial activity and can be further explored to confirm their suitability at clinical level.

Keywords: Pyrazole; Synthesis; Claisen-Schmidt condensation; Micheal addition; Antibacterial