| Author | Capelini, Camila | |
| Author | Câmara, Vitória R F | |
| Author | Villar, José D Figueroa | |
| Author | Barbosa, Juliana M C | |
| Author | Salomão, Kelly | |
| Author | Castro, Solange L de | |
| Author | Sales Junior, Policarpo Adhemar | |
| Author | Murta, Silvane Maria Fonseca | |
| Author | Couto, Thais B | |
| Author | Lourenço, Maria C S | |
| Author | Wardell, James L | |
| Author | Low, John N | |
| Author | Silva, Edson F da | |
| Author | Carvalho, Samir A | |
| Access date | 2022-03-24T18:39:23Z | |
| Available date | 2022-03-24T18:39:23Z | |
| Document date | 2021 | |
| Citation | CAPELINI, Camila et al. Synthesis, Antitrypanosomal and Antimycobacterial Activities of Coumarin N-acylhydrazonic Derivatives. Med Chem., v. 17, n. 6, p. 630-637, 2021. doi: 10.2174/1573406416666200121105215. | pt_BR |
| ISSN | 1573-4064 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/51867 | |
| Language | eng | pt_BR |
| Publisher | Bentham Science Publishers | pt_BR |
| Rights | restricted access | pt_BR |
| Title | Synthesis, Antitrypanosomal and Antimycobacterial Activities of Coumarin N-acylhydrazonic Derivatives | pt_BR |
| Type | Article | |
| DOI | 10.2174/1573406416666200121105215 | |
| 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. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Farmacos. Rio de Janeiro, RJ, Brazil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Farmacos. Rio de Janeiro, RJ, Brazil. | pt_BR |
| Affilliation | Instituto Militar de Engenharia. Departamento de Quimica. Grupo de Quimica Medicinal. Rio de Janeiro, RJ, Brazil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brazil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brazil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brazil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Rene Rachou. Belo Horizonte, MG, Brazil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Rene Rachou. Belo Horizonte, MG, Brazil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Rio de Janeiro, RJ, Brazil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Rio de Janeiro, RJ, Brazil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Farmacos. Rio de Janeiro, RJ, Brazil. | pt_BR |
| Affilliation | Department of Chemistry. University of Aberdeen. Old Aberdeen, Scotland, United Kingdom. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Farmacos. Rio de Janeiro, RJ, Brazil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Farmacos. Rio de Janeiro, RJ, Brazil | pt_BR |
| Subject | Antitrypanosomal | pt_BR |
| Subject | N-Acylhydrazone | pt_BR |
| Subject | antimycobacterial | pt_BR |
| Subject | chagas | pt_BR |
| Subject | coumarine | pt_BR |
| Subject | tuberculosis | pt_BR |
