European Journal of Chemistry

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

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Published: Jun 30, 2011
DOI: https://doi.org/10.5155/eurjchem.2.2.238-242.206
Keywords:
Isonicotinohydrazide, Pyrazol-5(H)-ones, Anti-tubercular activity, Anti-mycobacterial activity, Mycobacterium tuberculosis, M. tuberculosis H37Rv
Section
Research Article
Issue
Vol. 2 No. 2 (2011): June 2011
Dates
Received 2010-07-14
Accepted 2010-11-14
Published 2011-06-30


Main Article Content

Jignesh Priyakant Raval
Department of Pharmaceutical Chemistry, Ashok and Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences, New Vallabh Vidyanagar, Anand, Gujarat, 388121, India
Arpita Bharatbhai Shah
Department of Pharmaceutical Chemistry, Ashok and Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences, New Vallabh Vidyanagar, Anand, Gujarat, 388121, India
Nilesh Hasmukhbhai Patel
Department of Pharmaceutical Chemistry, Ashok and Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences, New Vallabh Vidyanagar, Anand, Gujarat, 388121, India
Hemul Venubhai Patel
Department of Pharmaceutical Chemistry, Ashok and Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences, New Vallabh Vidyanagar, Anand, Gujarat, 388121, India
Pradip Shantilal Patel
Department of Pharmaceutical Chemistry, Ashok and Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences, New Vallabh Vidyanagar, Anand, Gujarat, 388121, India
Kashyap Kanaiyalal Bhatt
Department of Pharmaceutical Chemistry, Indukaka Ipcowala College of Pharmacy, New Vallabh Vidyanagar, Anand, Gujarat, 38121, India
Kishor Ratilal Desai
C. G. Bhakta Institute of Biotechnology, Gopal Vidynagar, Tarsadi, Surat, Gujarat, 394350, India

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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(1)
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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