Synthesis and antimycobacterial evaluation of 3a,4-dihydro-3H-indeno [1,2-c] pyrazole-2-carboxamide analogues

  • Eur J Med Chem. 2011 Nov;46(11):5694-7. doi: 10.1016/j.ejmech.2011.09.035.
Mohamed Jawed Ahsan  1 ,  Jeyabalan Govinda Samy ,  Habibullah Khalilullah ,  Mohamed Afroz Bakht ,  Mohd Zaheen Hassan
Affiliations
  • 1. New Drug Discovery Research, Department of Medicinal Chemistry, Alwar Pharmacy College, Alwar, Rajasthan 301 030, India. [email protected]
PMID: 21978838 DOI: 10.1016/j.ejmech.2011.09.035
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 H(37)Rv 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, H(37)Rv and MDR-TB with minimum inhibitory concentrations 0.83 μM and 3.32 μM respectively.