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Research Article

Rational Design of Coumarin Derivatives as Antituberculosis Agents

, , , , , , & show all
Pages 2431-2444 | Received 14 Jan 2018, Accepted 14 Aug 2018, Published online: 16 Oct 2018
 

Abstract

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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Supplementary data

To view the supplementary data that accompany this paper please visit the journal website at: www.tandfonline.com/doi/full/10.4155/fmc-2018-0015

Author contributions

HM Mali has substantially contributed to the conception of idea; the acquisition, analysis and interpretation of data for the work and writing the manuscript. SS Sabale has contributed to acquisition of data, interpretation of work and writing manuscript. MS Degani has supervised the findings of this work and contributed to writing the manuscript. A Chaudhari, R Borkute have contributed for biological evaluation. D Sarkar supervised the findings of biological evaluationVS Krishna, D Sriram have contributed for antituberculosis activity against MtbH37Rv.

Financial & competing interests disclosure

HM Mali (201213-BSR-10398-137) and SS. Sabale are thankful to University Grants Commission India for providing financial support. A Choudhari is thankful to SERB, New Delhi for the award of N-PDF Fellowship. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.

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