2. Academic Validation
  3. 2-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: structural design, synthesis and pharmacological evaluation

2-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: structural design, synthesis and pharmacological evaluation

  • Eur J Med Chem. 2014 Oct 30:86:48-59. doi: 10.1016/j.ejmech.2014.08.012.
Marcos Veríssimo de Oliveira Cardoso 1,  Lucianna Rabelo Pessoa de Siqueira 2,  Elany Barbosa da Silva 2,  Lívia Bandeira Costa 2,  Marcelo Zaldini Hernandes 2,  Marcelo Montenegro Rabello 2,  Rafaela Salgado Ferreira 3,  Luana Faria da Cruz 3,  Diogo Rodrigo Magalhães Moreira 4,  Valéria Rêgo Alves Pereira 5,  Maria Carolina Accioly Brelaz de Castro 5,  Paul V Bernhardt 6,  Ana Cristina Lima Leite 2
Affiliations

Affiliations

  • 1 Departamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal de Pernambuco, 50740-520 Recife, PE, Brazil. Electronic address: marcosvocardoso@gmail.com.
  • 2 Departamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal de Pernambuco, 50740-520 Recife, PE, Brazil.
  • 3 Departamento de Bioquímica e Imunologia, Universidade Federal de Minas Gerais, CEP 31270-901 Belo Horizonte, MG, Brazil.
  • 4 Centro de Pesquisas Gonçalo Moniz, Fundação Oswaldo Cruz, CEP, 40296-750 Salvador, BA, Brazil.
  • 5 Centro de Pesquisas Aggeu Magalhães, Fundação Oswaldo Cruz, CEP, 50670-420 Recife, PE, Brazil.
  • 6 School of Chemistry and Molecular Biosciences, University of Queensland, Brisbane 4072, Australia.
PMID: 25147146 DOI: 10.1016/j.ejmech.2014.08.012
Abstract

The present work reports on the synthesis, anti-Trypanosoma cruzi activities and docking studies of a novel series of 2-(pyridin-2-yl)-1,3-thiazoles derived from 2-pyridine thiosemicarbazone. The majority of these compounds are potent cruzain inhibitors and showed excellent inhibition on the trypomastigote form of the Parasite, and the resulting structure-activity relationships are discussed. Together, these data present a novel series of thiazolyl hydrazones with potential effects against Chagas disease and they could be important leads in continuing development against Chagas disease.

Keywords

2-Pyridine thiosemicarbazone; Chagas disease; Hydrazones; Thiazoles; Trypanosoma cruzi.

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