Evaluation of structurally diverse benzoazepines clubbed with coumarins as Mycobacterium tuberculosis agents.
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 H(37) Rv 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 IC(50) 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.
Kuldip
K
Upadhyay
Atul
A
Manvar
Kena
K
Rawal
Sudhir
S
Joshi
Jalpa
J
Trivedi
Ravi
R
Chaniyara
Anamik
A
Shah
D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001381:Azepines / Q000737:chemistry*; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D021281:Quantitative Structure-Activity Relationship; D013841:Thiazepines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
D000995:Antitubercular Agents; D001381:Azepines; D003374:Coumarins; D013841:Thiazepines