Structure-activity relationship of natural and synthetic coumarin derivatives againstMycobacterium tuberculosis

Author(s)

Pires, Claudia T. A. ; Scodro, Regiane B. L. ; Cortez, Diogenes A. G. ; Brenzan, Mislaine A. ; Siqueira, Vera L. D. ; Caleffi-Ferracioli, Katiany R. ; Vieira, Lucas C. C. ; Monteiro, Julia L. ; Correa, Arlene G. ; Cardoso, Rosilene F.

• Document type: Journal article
• Source: Future Medicinal Chemistry; v. 12, n. 17, p. 14-pg., 2020-08-21.

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 againstMycobacterium tuberculosisH(37)Rv reference strain and multidrug-resistant clinical isolates.Materials & methods:Anti-M. tuberculosisactivity 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:Compounds1g,5,6,12and14were more active againstM. tuberculosisH(37)Rv and multidrug-resistant clinical isolates with minimum inhibitory concentration values ranging from 15.6 to 62.5 mu g/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. (AU)

• FAPESP's process: 14/50249-8 - Green chemistry: sustainable synthetic methods employing benign solvents, safer reagents, and bio-renewable feedstock
• Grantee: Arlene Gonçalves Corrêa
• Support Opportunities: Research Grants - Research Centers in Engineering Program
• FAPESP's process: 13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery
• Grantee: Glaucius Oliva
• Support Opportunities: Research Grants - Research, Innovation and Dissemination Centers - RIDC
• FAPESP's process: 15/17141-1 - Development and Mechanism Studies of New Synthetic Methodologies for the Synthesis of Bioactive Compounds.
• Grantee: Ricardo Samuel Schwab
• Support Opportunities: Regular Research Grants