DESIGN, SYNTHESIS, AND EVALUATION OF ANTIBACTERIAL POTENTIAL OF HYDRAZONE-TETHERED PYRAZOLE-THIAZOLE DERIVATIVES

Authors : Burak Kuzu, Aybek Yiğit, Fuat Karakuş

Pages : 42-52

Doi:10.33483/jfpau.1529096

View : 82 | Download : 78

Publication Date : 2025-01-20

Article Type : Research Paper

Abstract :Objective: This study includes the investigation of the antimicrobial potential of a series of compounds designed by hybridization of thiazole, hydrazone and pyrazole systems identified as antimicrobial moieties in the literature. The aim was to filter the designed compounds with drugability parameters, synthesize the selected compounds and test their antibacterial potential in silico and in vitro. Material and Method: The drugability properties of synthesized compounds were determined by online scanners and the potential effects of selected compounds on E. coli and S. aureus strains were determined by disk diffusion method. Also, Autodock 4.2 software was used to determine the inhibitory potential of compounds against the dihydrofolate reductase (DHFR) enzyme. Result and Discussion: In our study, among the newly designed hydrazone-linked pyrazole-thiazole compounds, the compounds determined according to their drugability parameters (17a-c) were synthesized with high efficiency. Among the compounds tested for antibacterial activity, Compound 17c formed a zone diameter of 8 mm against E. coli strain and 9 mm against S. aureus strain at a concentration of 80 μg/ml. Also, compound 17c formed a zone diameter of 7 mm against E. coli strain and 8 mm against S. aureus strain at a concentration of 40 μg/ml. Furthermore, the ADMET profiles of the presented compounds indicate that they may have suitable drugability parameters as potential antibacterial agents.
Keywords : Antibakteriyel, hibridizasyon, in siliko, sentez

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