Present address: Centre for Synthesis & Chemical Biology, School of Chemistry & Chemical Biology, University College Dublin, Belfield, Dublin 4, Ireland.
Evaluation of Structurally Diverse Benzoazepines Clubbed with Coumarins as Mycobacterium tuberculosis Agents
Article first published online: 12 OCT 2012
© 2012 John Wiley & Sons A/S
Chemical Biology & Drug Design
Volume 80, Issue 6, pages 1003–1008, December 2012
How to Cite
Upadhyay, K., Manvar, A., Rawal, K., Joshi, S., Trivedi, J., Chaniyara, R. and Shah, A. (2012), Evaluation of Structurally Diverse Benzoazepines Clubbed with Coumarins as Mycobacterium tuberculosis Agents. Chemical Biology & Drug Design, 80: 1003–1008. doi: 10.1111/j.1747-0285.2012.01436.x
- Issue published online: 25 OCT 2012
- Article first published online: 12 OCT 2012
- Accepted manuscript online: 21 JUN 2012 11:30AM EST
- Received 11 January 2012, revised 13 May 2012 and accepted for publication 5 June 2012
- microplate alamar blue assay;
Tuberculosis caused by Mycobacterium tuberculosis remains a leading cause of mortality worldwide into 21st century. In continuation with our anti-tuberculosis research programme, in this work, we have prepared molecularly diverse coumarins clubbed with benzothiazepines as well as its aza-analogues-benzodiazepines by molecular hybridization. The resulting compounds were screened for their M. tuberculosis activity against H37Rv strains using microplate alamar blue assay. Among the designed diversity, the compounds 5k, 5n and 5o were found significantly active in primary anti-tuberculosis assay at minimum inhibitory concentration <6.25 μm. Moreover, the IC50 values of 5k and 5o in level-2 screening were observed as >10 μg/mL and 3.63 μg/mL, respectively. Design and synthesis of more focused library and its three-dimensional quantitative structure activity relationship analysis are underway.