Evaluation of Structurally Diverse Benzoazepines Clubbed with Coumarins as Mycobacterium tuberculosis Agents |
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| Authors: | Kuldip Upadhyay Kena Rawal Sudhir Joshi Jalpa Trivedi Ravi Chaniyara Anamik Shah |
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| Affiliation: | 1. R & D Division, Gujarat Narmada Valley Fertilizers Company Limited, Narmadanagar‐392015, Gujarat, India;2. Alembic Research Centre, Alembic Pharmaceuticals Limited, Gujarat, Vadodara‐390003, India;3. Department of Chemistry, H & H. B. Kotak Science Institute, Rajkot‐360004, Gujarat, India;4. Department of Medicinal Chemistry, ISF College of Pharmacy, Moga‐142001, Punjab, India;5. New Drug Discovery Division, Wockhardt Research Centre, Aurangabad‐431136, Maharashtra, India;6. National Facility for Drug Discovery, Department of Chemistry, Saurashtra University, Rajkot‐360005, Gujarat, India |
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| Abstract: | 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. |
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| Keywords: | benzodiazepines benzothiazepines coumarins H37Rv microplate alamar blue assay Mtb |
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