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2-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: structural design, synthesis and pharmacological evaluation.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2014 Oct 30; Vol. 86, pp. 48-59. Date of Electronic Publication: 2014 Aug 06. - Publication Year :
- 2014
-
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.<br /> (Copyright © 2014 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Dose-Response Relationship, Drug
Molecular Structure
Parasitic Sensitivity Tests
Pyridines chemical synthesis
Pyridines chemistry
Structure-Activity Relationship
Thiazoles chemical synthesis
Thiazoles chemistry
Trypanocidal Agents chemical synthesis
Drug Design
Pyridines pharmacology
Thiazoles pharmacology
Trypanocidal Agents chemistry
Trypanocidal Agents pharmacology
Trypanosoma cruzi drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 86
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 25147146
- Full Text :
- https://doi.org/10.1016/j.ejmech.2014.08.012