European Journal of Chemistry

Synthesis and anti-tubercular activity of novel pyrazol-5(H)-one derivatives



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Jignesh Priyakant Raval
Arpita Bharatbhai Shah
Nilesh Hasmukhbhai Patel
Hemul Venubhai Patel
Pradip Shantilal Patel
Kashyap Kanaiyalal Bhatt
Kishor Ratilal Desai

Abstract

In the present investigation, a series of 1-isonicotinoyl-3-methyl-4-(2-(substituted-phenyl)hydrazono)-1H-pyrazol-5(H)-ones were synthesized by the reaction between isonicotinohydrazide with substituted ethylacetoacetate derivatives using acetic acid as solvent which yielded substituted pyrazol-5(H)-one derivatives. Newly synthesized compounds were tested for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system. Among the synthesized compounds, 4-(2-(2,6-dichlorophenyl)hydrazono)-1-isonicotinoyl-3-methyl-1H-pyrazol-5(4H)-one and 4-(2-(1-isonicotinoyl-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl) benzene-sulfonamide were found to be more active agent against M. tuberculosis H37Rv with minimum inhibitory concentration of 0.0034, 0.0032 µM at actual MIC 1.66 and 1.64 µg/mL, respectively.

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Raval, J. P.; Shah, A. B.; Patel, N. H.; Patel, H. V.; Patel, P. S.; Bhatt, K. K.; Desai, K. R. Synthesis and Anti-Tubercular Activity of Novel Pyrazol-5(H)-One Derivatives. Eur. J. Chem. 2011, 2, 238-242.

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