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Published on: December 4, 2016
Rational design of coumarin derivatives as antituberculosis agents
Hemlata M Mali1, Sandip S Sabale1, Mariam S Degani1
1Department of Pharmaceutical Sciences & Technology, Institute of Chemical Technology, Matunga (E), Mumbai 400019, India.
Aim:
A series of coumarin derivatives was designed as potential antituberculosis agents.
Results:
The compounds were screened against active and dormant Mycobacterium tuberculosis (Mtb). Compounds 3k and 3n were found to have the most promising activity against replicating MtbH37Rv exhibiting minimum inhibitory concentration of 4.63 and 9.75 μM respectively. The compounds were also effective against dormant MtbH37Rv exhibiting more potency than the standard drugs, isoniazid and rifampicin. The compounds were found to be non-cytotoxic against human cell lines.
Conclusion:
This study provides promising antituberculosis agents that are effective against replicating as well as dormant Mtb and can thus act as potential leads for further development.
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