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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. Sales Junior, Silvane M. F. Murta, Thais B. Couto, Maria Cristina S. Lourenço, James L. Wardell, John N. Low, Edson F. da Silva and Samir A. Carvalho*   Pages 1 - 8 ( 8 )

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 to this disease.

Method: We reported herein the synthesis, antitrypanosomal and antimycobacterial activities of seventeen coumarinic N-acylhydrazonic derivatives.

Results: These compounds were synthesized using methodology with reactions global yields ranging from 46%-70%. T. cruzi in vitro effect were evaluated against trypomastigote and amastigote forms and M. tuberculosis activity were 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

Affiliation:

Instituto de Tecnologia em Fármacos - Farmanguinhos, Fundação Oswaldo Cruz, 21041-250 Rio de Janeiro, RJ, Instituto de Tecnologia em Fármacos - Farmanguinhos, Fundação Oswaldo Cruz, 21041-250 Rio de Janeiro, RJ, Grupo de Química Medicinal, Departamento de Química, Instituto Militar de Engenharia, Praça General Tibúrcio 80, 22290-270 Rio de Janeiro, Laboratório de Biologia Celular, Instituto Oswaldo Cruz, Fundação Oswaldo Cruz, 21040-900, Rio de Janeiro, RJ, Laboratório de Biologia Celular, Instituto Oswaldo Cruz, Fundação Oswaldo Cruz, 21040-900, Rio de Janeiro, RJ, Laboratório de Biologia Celular, Instituto Oswaldo Cruz, Fundação Oswaldo Cruz, 21040-900, Rio de Janeiro, RJ, Instituto René Rachou - Fundação Oswaldo Cruz, 30190002 - Belo Horizonte, MG , Instituto René Rachou - Fundação Oswaldo Cruz, 30190002 - Belo Horizonte, MG , Instituto Nacional de Infectologia Evandro Chagas, Fundação Oswaldo Cruz, 21045-900 Rio de Janeiro, RJ, Instituto Nacional de Infectologia Evandro Chagas, Fundação Oswaldo Cruz, 21045-900 Rio de Janeiro, RJ, Instituto de Tecnologia em Fármacos - Farmanguinhos, Fundação Oswaldo Cruz, 21041-250 Rio de Janeiro, RJ, Department of Chemistry, University of Aberdeen, Old Aberdeen, AB 24 3 UE, Scotland, Instituto de Tecnologia em Fármacos - Farmanguinhos, Fundação Oswaldo Cruz, 21041-250 Rio de Janeiro, RJ, Instituto de Tecnologia em Fármacos - Farmanguinhos, Fundação Oswaldo Cruz, 21041-250 Rio de Janeiro, RJ



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