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Synthesis and antimycobacterial evaluation of 3a,4-dihydro-3H-indeno [1,2-c] pyrazole-2-carboxamide analogues
Authors:Ahsan Mohamed Jawed  Samy Jeyabalan Govinda  Khalilullah Habibullah  Bakht Mohamed Afroz  Hassan Mohd Zaheen
Affiliation:aNew Drug Discovery Research, Department of Medicinal Chemistry, Alwar Pharmacy College, Alwar, Rajasthan 301 030, India;bDepartment of Pharmaceutical Sciences, National Institute of Medical Sciences University, Jaipur 303 121, India;cDepartment of Pharmaceutical Chemistry, College of Pharmacy in Al-Kharj University, P.O. Box 11323, Saudi Arabia;dDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard University, New Delhi 110 062, India
Abstract:
In the present investigation, a series of 3a,4-dihydro-3H-indeno [1,2-c] pyrazole-2-carboxamide analogues were synthesized and were evaluated for antitubercular activity by two fold serial dilution technique. All the newly synthesized compounds showed low to good inhibitory activities against Mycobacterium tuberculosis H37Rv and multi-drug resistant M. tuberculosis (MDR-TB). 3-(4-fluorophenyl)-N-(4-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 MDR-TB with minimum inhibitory concentrations 0.83 μM and 3.32 μM respectively.
Keywords:Pyrazolines   Antitubercular agents   Mycobacterium tuberculosis   Multi-drug resistant tuberculosis
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