Saturday, September 7, 2013

Studies on substituted benzo[h]quinazolines, benzo[g]indazoles, pyrazoles, 2,6-diarylpyridines as anti-tubercular agents

Bioorganic & Medicinal Chemistry Letters,  Volume 23, Issue 21, 1 November 2013, Pages 5844–5849Available online 5 September 2013
Hardesh KMaurya, Ruby Verma, Saba Alam, Shweta Pandey, Vinay Pathak, Sandeep Sharma, Kishore K. Srivastava, Arvind S. Negi, Atul Gupta
http://dx.doi.org/10.1016/j.bmcl.2013.08.101
Abstract
Various substituted 5,6-dihydro-8-methoxybenzo[h]quinazolin-2-amine, 1-(3-(4-alkoxyphenyl)-7-methoxy-3,3a,4,5-tetrahydro-2H benzo[g]indazol-2-yl)ethanone, pyrazole and 2,6-diarylpyridine derivatives have been synthesized in good yields by an efficient methodology. The synthesized compounds (4-23) were evaluated for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain. Compounds 6a,6c8a, 19a and 19e exhibited significant anti-tubercular activity at MIC values 50, 100, 50, 25 and 100 μM concentration. In vitro cytotoxicity data using THP-1 cells indicated that most active compound 19a is safe as its MIC value is much lower than the cytotoxic value.