Molecular Properties Prediction and Synthesis of Novel Pyrazoline Carboxamide Analogs as Antitubercular Agents

ISSN: 2211-3533 (Online)
ISSN: 2211-3525 (Print)


Volume 14, 2 Issues, 2016


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Anti-Infective Agents

Formerly: Anti-Infective Agents in Medicinal Chemistry

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Molecular Properties Prediction and Synthesis of Novel Pyrazoline Carboxamide Analogs as Antitubercular Agents



Anti-Infective Agents, 10(2): 117-123.

Author(s): Mohamed Jawed Ahsan, Jeyabalan Govinda Samy, Habibullah Khalilullah, Choudhary R. Kirit and Savita Soni.

Affiliation: Department of Pharmaceutical Sciences, National Institute of Medical Sciences University, Jaipur 303 121, India.

Abstract

In the present investigation, a series of 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2- c]pyrazole-2-carboxamide analogs were synthesized based on the structure of known antitubercular drug thiacetazone and were evaluated for antitubercular activity by two fold serial dilution technique. A computational study was carried out for prediction of pharmacokinetic properties and none of the compounds violated Lipinski “Rule of Five”. The structures of the synthesized compounds were confirmed on the basis of their spectral data and elemental analysis. All the newly synthesized compounds showed low to good activity inhibitory activities against Mycobacterium tuberculosis H37Rv (MTB) and isoniazid resistant M. tuberculosis (INHR-MTB). 3-(4-fluoromethyl)-N-(2-chlorophenyl)-6,7-dimethoxy-3a,4- dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide (4c) was found to be the most promising compound active against M. tuberculosis H37Rv and isoniazid resistant M. tuberculosis (INHR-MTB) with minimum inhibitory concentration 0.83 and 3.35 μM respectively.

Keywords:

Pyrazolines, claisen schmidt condensation, antitubercular agents, molecular properties prediction, lipophilicity; lipinski “rule of five”.



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Article Details

Volume: 10
Issue Number: 2
First Page: 117
Last Page: 123
Page Count: 7
DOI: 10.2174/2211362611208020117
Price: $58
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