Mabilly Cox Holanda de Barros Dias, Mayara Souza Barbalho, Gevanio Bezerra de Oliveira Filho, Marcos Veríssimo de Oliveira Cardoso, Ana Cristina Lima Leite, Aline Caroline da Silva Santos, Ana Catarina Cristovão Silva, Maria Carolina Accioly Brelaz de Castro, Danielle Maria Nascimento Moura, Luiz Felipe Gomes Rebello Ferreira, Marcelo Zaldini Hernandes, Rafael de Freitas E Silva, Valéria Rêgo Alves Pereira
Chagas disease is a deadly and centenary neglected disease that is recently surging as a potential global threat. Approximately 30% of infected individuals develop chronic Chagas cardiomyopathy and current treatment with the reference benznidazole (BZN) is ineffective for this stage. We presently report the structural planning, synthesis, characterization, molecular docking prediction, cytotoxicity, in vitro bioactivity and mechanistic studies on the anti-T. cruzi activity of a series of 16 novel 1,3-thiazoles (2-17) derived from thiosemicarbazones (1a, 1b) in a two-step and reproducible Hantzsch-based synthesis approach...
May 19, 2023: European Journal of Medicinal Chemistry