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

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.

• Authors: Marcos Veríssimo de Oliveira Cardoso, Lucianna Rabelo Pessoa de Siqueira, Elany Barbosa da Silva, Lívia Bandeira Costa, Marcelo Zaldini Hernandes, Marcelo Montenegro Rabello, Rafaela Salgado Ferreira, Luana Faria da Cruz, Diogo Rodrigo Magalhães Moreira, Valéria Rêgo Alves Pereira, Maria Carolina Accioly Brelaz de Castro, Paul V Bernhardt, Ana Cristina Lima Leite
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 86 Pg. 48-59 (Oct 30 2014) ISSN: 1768-3254 [Electronic] France
• PMID: 25147146 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Chemical References

• Pyridines
• Thiazoles
• Trypanocidal Agents

Topics

• Dose-Response Relationship, Drug
• Drug Design
• Molecular Structure
• Parasitic Sensitivity Tests
• Pyridines (chemical synthesis, chemistry, pharmacology)
• Structure-Activity Relationship
• Thiazoles (chemical synthesis, chemistry, pharmacology)
• Trypanocidal Agents (chemical synthesis, chemistry, pharmacology)
• Trypanosoma cruzi (drug effects)