Antitubercular Activity and Synergistic Study of Novel Pyrazole Derivatives

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Abstract

A series of 20 novel pyrazole derivatives were designed and prepared, characterized by 1H-NMR, mass spectra (ES-MS), 13C-NMR, and elemental analysis. The synthesized compounds were then evaluated for their growth inhibitory activity against Mycobacterium smegmatis mc2 155 initially. Rifampicin was used as standard reference. In this screening, derivatives 9, 10, and 11 presented superior inhibition compared with standard. Later, these three compounds were exposed for their Mycobacterium tuberculosis H37Rv inhibitory assay using rifampicin as standard reference. Encouraging M. smegmatis mc2 155 inhibition (9 μg/mL), M. tuberculosis H37Rv inhibition (1.9 μg/mL), and synergism with the first-line and second-line antibiotics made compound 10 as lead and safe antitubercular agent among the series.

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Jadhav, S. B., Fatema, S., Sanap, G., & Farooqui, M. (2018). Antitubercular Activity and Synergistic Study of Novel Pyrazole Derivatives. Journal of Heterocyclic Chemistry, 55(7), 1634–1644. https://doi.org/10.1002/jhet.3198

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