2-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: Structural design, synthesis and pharmacological evaluation
| Autor: | Rafaela Salgado Ferreira, Lucianna Rabelo Pessoa de Siqueira, Marcos Veríssimo de Oliveira Cardoso, Valéria Rêgo Alves Pereira, Maria Carolina Accioly Brelaz de Castro, Marcelo M. Rabello, Elany Barbosa da Silva, Diogo Rodrigo Magalhães Moreira, Luana Faria da Cruz, Paul V. Bernhardt, Ana Cristina Lima Leite, Marcelo Zaldini Hernandes, Lívia Bandeira Costa |
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| Rok vydání: | 2014 |
| Předmět: |
Pharmacology
Chagas disease Dose-Response Relationship Drug Molecular Structure biology Pyridines Chemistry Trypanosoma cruzi Organic Chemistry General Medicine medicine.disease biology.organism_classification Trypanocidal Agents Structure-Activity Relationship Thiazoles Parasitic Sensitivity Tests Biochemistry Design synthesis Docking (molecular) Drug Design Drug Discovery medicine |
| Zdroj: | European Journal of Medicinal Chemistry. 86:48-59 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2014.08.012 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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