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  • Title: Structure-activity relationship of natural and synthetic coumarin derivatives against Mycobacterium tuberculosis.
    Author: Pires CT, Scodro RB, Cortez DA, Brenzan MA, Siqueira VL, Caleffi-Ferracioli KR, Vieira LC, Monteiro JL, Corrêa AG, Cardoso RF.
    Journal: Future Med Chem; 2020 Sep; 12(17):1533-1546. PubMed ID: 32820960.
    Abstract:
    Aim: Eight coumarin derivatives (1a-h) obtained from natural (-)-mammea A/BB (1) and 13 synthetic coumarins (2-14) had their cytotoxicity and biological activity evaluated against Mycobacterium tuberculosis H37Rv reference strain and multidrug-resistant clinical isolates. Materials & methods: Anti-M. tuberculosis activity was evaluated by resazurin microtiter assay plate, and the cytotoxicity of natural and synthetic products using J774A.1 macrophages by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide. Results: Compounds 1g, 5, 6, 12 and 14 were more active against M. tuberculosis H37Rv and multidrug-resistant clinical isolates with MIC values ranging from 15.6 to 62.5 μg/ml. Conclusion: These results demonstrate that the coumarin derivatives were active against multidrug-resistant clinical isolates, becoming potential candidates to be used in the treatment of resistant tuberculosis.
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