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

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.

2_2_238_242_800


Keyword(s)


Isonicotinohydrazide; Pyrazol-5(H)-ones; Anti-tubercular activity; Anti-mycobacterial activity; Mycobacterium tuberculosis; M. tuberculosis H37Rv

European Journal of Chemistry, 2 (2), (2011), 238-242

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DOI: http://dx.doi.org/10.5155/eurjchem.2.2.238-242.206