SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL ACTIVITY OF SOME NOVEL 3,4-DISUBSTITUTED PYRAZOLE DERIVATIVES

  • GANESH AKULA Department of Pharmacy, Mewar University, Chittorgarh, Rajasthan, India.
  • KAUSHAL K CHANDRUL Department of Pharmacy, Mewar University, Chittorgarh, Rajasthan, India.
  • BHIKSHAPATHI DVRN Department of Pharmacy, Mewar University, Chittorgarh, Rajasthan, India.

Abstract

Objective: The objective of the current work was to synthesize a series of 3,4-substituted pyrazoles from the cyclization of substituted aryl ethanone and hydrazine hydrate in a two-step process and screen the derivatives for their antimicrobial activity.


Methods: The title compounds were derived from the condensation of ethanone intermediate with N, N-Dimethyl formamide-dimethyl acetal and hydrazine hydrate. Ethanone intermediate synthesized from substituted methyl phenylacetate in the presence of potassium t-butoxide with 6-methyl pyridine-2-carboxylic acid methyl ester.


Results: The final products were characterized by detailed spectral analysis using Mass, Nuclear Magnetic Resonance, and Infra Red spectroscopy. All the compounds (4a-4j) showed significant antibacterial properties on both Gram-positive and Gram-negative bacteria. Interestingly, the selected microbes were found to be highly sensitive for compound 4a, 4c, 4d, 4h, and 4i. The molecules are also antifungal in nature, and they have a significant inhibitory effect on the growth of Candida albicans and Aspergillus niger.


Conclusion: The results suggest that the developed derivatives bearing the pyrazole nucleus could be the lead structures for the development of antimicrobial agents for fatal infections.

Keywords: Pyrazoles, Condensation, Antibacterial, Antifungal

Author Biography

GANESH AKULA, Department of Pharmacy, Mewar University, Chittorgarh, Rajasthan, India.

Associate professor,

Department of Pharmaceutical Chemistry

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GANESH AKULA, KAUSHAL K CHANDRUL, and BHIKSHAPATHI DVRN. “SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL ACTIVITY OF SOME NOVEL 3,4-DISUBSTITUTED PYRAZOLE DERIVATIVES”. Asian Journal of Pharmaceutical and Clinical Research, Vol. 13, no. 1, Nov. 2019, pp. 129-33, doi:10.22159/ajpcr.2020.v13i1.36216.
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