Volume : 09, Issue : 07, July – 2022
08.SYNTHESIS, CHARACTERIZATION AND PHARMACOLOGICAL EVALUATION OF NOVEL ISOXAZOLE BEARING PYRAZOLE DERIVATIVES FOR ANTIBACTERIAL ACTIVITY
Kamlesh Kumar Pandey, Alok Pal Jain, Amit Nayak*
Objective: The objective of the paper was to synthesis and characterization of new isoxazole bearing pyrazole derivatives and evaluate them for antibacterial activity.
Material and methods: The isoxazole bearing pyrazole derivatives have been synthesized by the utilize the four-step process. Total Ten compounds have been synthesized and characterized by IR, 1HNMR, elemental and mass spectral analysis. The final compounds (PIA-1 to PIA-10) have been evaluated for antibacterial activity by disk diffusion method using sulfamethoxazole as standard drug.
Result and Discussion: The IR spectra of compound PIA-1 to PIA-10 shown the characteristics peak at 3052 (N-H), 2964 (C-H), 1628 (C=O), 1448 (C=N), 1625 (C=C), 1126 (C-O); 1015 (C-Br); 850 (C-Cl) and 1102 (C-F). The 1HNMR spectrum show the characteristics peak δ 6.68-6.70 (d, 2H, Ar-Fluorine), 7.14-7.16 (d, 1H, Ar-chlorine), 7.28-7.30 (m, 5H, Ar-H), 7.58-8.00 (d, 2H, Ar-Chlorine), 7.75-7.78 (d, 2H, Ar-Fluorine), 8.25 (s, 1H, Ar-H isoxazole), 10.97 (s, 1H, -Ar-H pyrazole); 7.26 (s, 1H, Ar-Cl). The antibacterial evaluation of the synthesized compounds stated that Isoxazole-pyrazole derivatives exhibit considerable inhibitory effect on all bacteria strains at both 50 µg/ml and 100 µg/ml dosing levels. PIA-1, PIA-2, PIA-3, PIA-4 had the highest activity in gram positive bacterial stains and PIA-1, PIA-3, PIA-4 and PIA-10 have shown best activity against gram negative bacteria.
Conclusion: The antibacterial activity of the synthesized compounds (PIA-1, PIA-3, PIA-4 and PIA-5) was significantly similar or better than that of standard Drug used for comparison. These Isoxazole bearing pyrazole compounds have demonstrated potency as a superior antibacterial agent, although more in-vivo research on the efficacy and dosage regimen of the compounds is needed.
Keywords: Antibacterial activity, Pyrazole, Isoxazole, sulfamethoxazole, disk diffusion
Cite This Article:
Please cite this article in press Kamlesh Kumar Pandey et al, Synthesis, Characterization And Pharmacological Evaluation Of Novel Isoxazole Bearing Pyrazole Derivatives For Antibacterial Activity., Indo Am. J. P. Sci, 2022; 09(7).,
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