Mohammad Firoj Khan and Ketkee Mandawar
In this study, chalcones and pyrazoline derivatives were synthesized and evaluated for their multifarious pharmacological profiles, particularly their antimicrobial and antimalarial activities. The synthesis of compounds 3a-3p and 4a-4p was achieved through the Claisen-Schmidt reaction and subsequent reactions with nicotinic acid hydrazide, yielding products with high purity and anticipated structures confirmed by physico-chemical characterization methods including FT-IR, 1H-NMR, mass spectral, and elemental analyses. The compounds displayed solubility in various organic solvents but were insoluble in water. Antimicrobial activity assays against Gram-positive and Gram-negative bacteria, as well as antifungal activity tests, demonstrated that several compounds exhibited mild to good activity. Notably, compounds 4d, 4h, 4l, 4n, and 4p showed significant antibacterial activity, while 4i, 4k, 4l, and 4p were most effective against fungi. Furthermore, the in vitro antimalarial activity identified compound 4p as the most promising candidate. Compounds 4d and 4p are highlighted as potential leads for further analog synthesis and structure-activity relationship studies to enhance antimicrobial efficacy. These findings suggest promising directions for the development of new therapeutic agents based on chalcone and pyrazoline scaffolds.
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