1417540-53-4Relevant academic research and scientific papers
Evaluation of Structurally Diverse Benzoazepines Clubbed with Coumarins as Mycobacterium tuberculosis Agents
Upadhyay, Kuldip,Manvar, Atul,Shah, Anamik,Rawal, Kena,Joshi, Sudhir,Trivedi, Jalpa,Chaniyara, Ravi
, p. 1003 - 1008,6 (2012/12/12)
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 50 values of 5k and 5o in level-2 screening were observed as >10μg/mL and 3.63μg/mL, respectively. Design and synthesis of more focused library and its three-dimensional quantitative structure activity relationship analysis are underway. In the present work, various coumarins clubbed with benzo(thi)diazepines were evaluated for their M. tuberculosis activity against H37Rv strains using MABA assay. The IC50 values of two analogs (compounds 5k and 5o) in level-2 screening were observed as >10μg/mL and 3.63μg/mL respectively.
