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

Veríssimo de Oliveira Cardoso, Marcos, Pessoa de Siqueira, Lucianna Rabelo, Barbosa da Silva, Elany, Bandeira Costa, Lívia, Zaldini Hernandes, Marcelo, Montenegro Rabello, Marcelo, Salgado Ferreira, Rafaela, Faria da Cruz, Luana, Rodrigo Magalhaes Moreira, Diogo, Rego Alves Pereira, Valeria, Accioly Brelaz de Castro, Maria Carolina, Bernhardt, Paul V. and Lima Leite, Ana Cristina (2014) 2-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: structural design, synthesis and pharmacological evaluation. European Journal of Medicinal Chemistry, 86 48-59. doi:10.1016/j.ejmech.2014.08.012

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Author Veríssimo de Oliveira Cardoso, Marcos
Pessoa de Siqueira, Lucianna Rabelo
Barbosa da Silva, Elany
Bandeira Costa, Lívia
Zaldini Hernandes, Marcelo
Montenegro Rabello, Marcelo
Salgado Ferreira, Rafaela
Faria da Cruz, Luana
Rodrigo Magalhaes Moreira, Diogo
Rego Alves Pereira, Valeria
Accioly Brelaz de Castro, Maria Carolina
Bernhardt, Paul V.
Lima Leite, Ana Cristina
Title 2-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: structural design, synthesis and pharmacological evaluation
Formatted title
2-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: structural design, synthesis and pharmacological evaluation 
Journal name European Journal of Medicinal Chemistry   Check publisher's open access policy
ISSN 0223-5234
1768-3254
Publication date 2014-10-30
Sub-type Article (original research)
DOI 10.1016/j.ejmech.2014.08.012
Volume 86
Start page 48
End page 59
Total pages 12
Place of publication Issy les Moulineaux, Cedex, France
Publisher Elsevier Masson
Collection year 2015
Language eng
Formatted 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.
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2015 Collection
School of Chemistry and Molecular Biosciences
 
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Citation counts: TR Web of Science Citation Count  Cited 15 times in Thomson Reuters Web of Science Article | Citations
Scopus Citation Count Cited 19 times in Scopus Article | Citations
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Created: Fri, 29 Aug 2014, 23:50:55 EST by Mrs Louise Nimwegen on behalf of School of Chemistry & Molecular Biosciences