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.
Highlights
Various substituted pyrazole based drugs are acquiring significance in medicinal and natural products research by virtue of its multifarious properties and broad spectrum of applications for various ailments [1]
Since the foundation of the primary synthetic method of pyrazole, i.e., Paal–Knorr synthesis by condensation of 1,3-diketones with hydrazine which yields substituted pyrazoles, it is the subject matter for investigators to create the substituted pyrazoles
Various substituted pyrazole derivatives have been synthesized in a two-step process involving the cyclization of ethenone intermediate with hydrazine moiety
Summary
Various substituted pyrazole based drugs are acquiring significance in medicinal and natural products research by virtue of its multifarious properties and broad spectrum of applications for various ailments [1]. The abundant texts support the ubiquitous nature of aza-heterocyclic compounds, the pyrazole derivatives. They are documented to possess anticancer [2,3,4], antibacterial [5], antifungal [6,7], antitubercular [8,9], analgesic [10,11], antimalarial [12,13], antipyretic [14], anticonvulsant [15], antidepressant [16], antiangiogenetic [17], antidiabetic [18], antiviral [19,20], and antiinflammatory [21,22,23] activities. To overwhelm the severe reaction conditions and to have regioselectivity, a basic and beneficial strategy was utilized for the synthesis of substituted pyrazoles
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