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Article Synthesis and Trypanocidal Activity of Novel 2,4,5-Triaryl-N-Hydroxylimidazole Derivatives

Authors :
Edson Ferreira da Silva
James L. Wardell
Solange M. S. V. Wardell
Carlos A. M. Fraga
Kelly Salomão
Vanessa Brandão Loback
Carmen Penido
Thadeu Estevam Moreira Maramaldo Costa
Samir A. Carvalho
Solange L. de Castro
Maria das Graças Henriques
Ramon Silva
Source :
Molecules, Molecules, Vol 18, Iss 3, Pp 3445-3457 (2013), Molecules; Volume 18; Issue 3; Pages: 3445-3457
Publication Year :
2013
Publisher :
MDPI AG, 2013.

Abstract

Herein, we report the design, synthesis and trypanocidal activity of some novel trisubstituted imidazole derivatives. These heterocyclic derivatives were structurally planned by exploring the concept of molecular hybridisation between two arylhydrazones derived from megazol, which has potent trypanocidal activity. The trypanocidal activity of these triarylimidazole derivatives was evaluated against infective trypomastigote forms of T. cruzi and the derivative 2'-(4-bromophenyl)-1-methyl-5'-phenyl-1H,3'H-2,4'-biimidazol-3'-ol showed moderate biological activity (IC50 = 23.9 µM) when compared to benznidazole, a standard trypanocidal drug. These compounds did not present cytotoxic effects at concentrations near the trypanocidal IC50, being considered a good starting point for the development of new anti-Chagas drug candidates.

Details

ISSN :
14203049
Volume :
18
Database :
OpenAIRE
Journal :
Molecules
Accession number :
edsair.doi.dedup.....990c768abba9e65a90f06b0eda9a1516
Full Text :
https://doi.org/10.3390/molecules18033445