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Medicinal Chemistry

Author(s): Camila Capelini, Vitória R.F. Câmara, José D. Figueroa Villar, Juliana M.C. Barbosa, Kelly Salomão, Solange L. de Castro, Policarpo A.S. Junior, Silvane M.F. Murta, Thais B. Couto, Maria C.S. Lourenço, James L. Wardell, John N. Low, Edson F. da Silva and Samir A. Carvalho*

DOI: 10.2174/1573406416666200121105215

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Synthesis, Antitrypanosomal and Antimycobacterial Activities of Coumarin N-acylhydrazonic Derivatives

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Abstract

Background: Near to 5-7 million people are infected with T. cruzi in the world, and about 10,000 people per year die of problems associated with this disease.

Methods: Herein, the synthesis, antitrypanosomal and antimycobacterial activities of seventeen coumarinic N-acylhydrazonic derivatives have been reported.

Results: These compounds were synthesized using methodology with reactions global yields ranging from 46%-70%. T. cruzi in vitro effects were evaluated against trypomastigote and amastigote, forming M. tuberculosis activity towards H37Rv sensitive strain and resistant strains.

Discussion: Against T. cruzi, the more active compounds revealed only moderate activity IC50/96h~20 μM for both trypomastigotes and amastigotes intracellular forms. (E)-2-oxo-N'- (3,4,5-trimethoxybenzylidene)-2H-chromene-3-carbohydrazide showed meaningful activity in INH resistant/RIP resistant strain.

Conclusion: These compound acting as multitarget could be good leads for the development of new trypanocidal and bactericidal agents.

Keywords: Antitrypanosomal, antimycobacterial, coumarine, N-Acylhydrazone, chagas, tuberculosis.

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