New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi.
Basic Information
ID: ALA4715737
Journal: Eur J Med Chem
Title: New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi.
Authors: de Moraes Gomes PAT,de Oliveira Barbosa M,Farias Santiago E,de Oliveira Cardoso MV,Capistrano Costa NT,Hernandes MZ,Moreira DRM,da Silva AC,Dos Santos TAR,Pereira VRA,Brayner Dos Santosd FA,do Nascimento Pereira GA,Ferreira RS,Leite ACL
Abstract: In previous studies, the compound 3-(bromopropiophenone) thiosemicarbazone was described as a potent anti-Trypanosoma cruzi and cruzain inhibitor. In view to optimize this activity, 1,3-thiazole core was used as building-block strategy to access new lead generation of anti T. cruzi agents. In this way a series of thiazole derivatives were synthesized and most of these derivatives exhibited antiparasitic activity similar to benznidazole (Bzd). Among them, compounds (1c) and (1g) presented better selective index (SI) than Bzd. In addition, compounds showed inhibitory activity against the cruzain protease. As observed by electron microscopy, compound (1c) treatment caused irreversible and specific morphological changes on ultrastructure organization of T. cruzi, demonstrating that this class of compounds is killing parasites.
CiteXplore: 27295485
DOI: 10.1016/j.ejmech.2016.05.050
Patent ID: ┄