Discovery of novel antitubercular 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues

作者：Ahsan Mohamed Jawed^*; Samy Jeyabalan Govinda; Soni Savita; Jain Naresh; Kumar Lalit; Sharma Lalit K; Yadav Hemant; Saini Lokesh; Kalyansing Rajput Gopal; Devenda Narendra S; Prasad Ravindra; Jain Chandra Bhushan

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(18): 5259-5261.

DOI：10.1016/j.bmcl.2011.07.035

• Pyrazolines
• Antitubercular agents

In the present investigation, a series of 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues were synthesized and were evaluated for antitubercular activity by two fold serial dilution technique. All the newly synthesized compounds showed low to high inhibitory activities against Mycobacterium tuberculosis H(37)Rv and INH resistant M. tuberculosis. The compound 3-(4-fluorophenyl)-6,7-dimethoxy-3a, 4-dihydro-3H-indeno[1,2-c]pyrazole-2-carbothioamide (4o) was found to be the most promising compound active against M. tuberculosis H(37)Rv and isoniazid resistant M. tuberculosis with minimum inhibitory concentration 3.12 mu M and 6.25 mu M, respectively.

• 出版日期2011-9-15
• 单位河北医科大学