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

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, Samir A. Carvalho*

Journal Name: Medicinal Chemistry

Volume 17 , Issue 6 , 2021


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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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Article Details

VOLUME: 17
ISSUE: 6
Year: 2021
Published on: 08 June, 2021
Page: [630 - 637]
Pages: 8
DOI: 10.2174/1573406416666200121105215
Price: $65

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