Facing chagas' disease: Trypanocidal properties of new coumarinchalcone scaffolds

• Tipo: Artigo em Revista Científica Internacional
• Data: 2016

Autores

Vazquez Rodriguez, S (Autor) Outra; Guíñez, RF (Autor) Outra; Matos, MJ (Autor) Outra; Olea Azar, C (Autor) Outra; Maya, JD (Autor) Outra; Uriarte, E (Autor) Outra; Santana, L (Autor) Outra

Revista

Título: Medicinal Chemistry

Vol. 12

Páginas: 537-543

ISSN: 1573-4064

Editora: Bentham Science

Indexação

Scopus - 3 Citações

Outras Informações

ID Authenticus: P-00R-0NB

DOI: 10.2174/1573406412666160107111809

Abstract (EN): With the aim of finding new chemical entities based on coumarin and chalcone scaffolds, new hybrid compounds 2-5 were designed and synthesized. The trypanocidal activity of these compounds was tested against the epimastigote, trypomastigote and amastigote stages of the Trypanosoma cruzi parasite. Cytotoxicity assays were also performed in RAW 264.7 and VERO cells. Compound 5 presented the highest trypanocidal activity of the series, with trypanocidal values higher than nifurtimox for the trypomastigote and epimastigote stages., but presenting cytotoxic effects in the mammalian cells. A SAR study suggested that methoxy substitution at positions 2 and 5 in the designed scaffold seemed to be a key feature for the trypanocidal activity. Therefore, the coumarin-chalcone scaffold can be taken into account for further lead optimization and design new and more effective trypanocidal compounds. © 2016 Bentham Science Publishers.

Idioma: Inglês

Tipo (Avaliação Docente): Científica