Next Article in Journal
Bioactive Pregnane Steroids from a South China Sea Gorgonian Carijoa sp.
Previous Article in Journal
Remarks on Sasidharan et al. “Evaluation of the Hepatoprotective Effects of Lantadene A, a Pentacyclic Triterpenoid of Lantana Plants against Acetaminophen-induced Liver Damage”. Molecules 2012, 17, 13937-13947
Molecules 2013, 18(3), 3445-3457; doi:10.3390/molecules18033445
Article

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

1,2
,
1
,
3
,
3
,
4
,
5
,
1
,
1
,
1
,
1
,
1
 and
2,6,*
Received: 7 February 2013 / Revised: 25 February 2013 / Accepted: 8 March 2013 / Published: 15 March 2013
Download PDF [266 KB, uploaded 18 June 2014]

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.
Keywords: 2,4,5-triaryl-N-hydroxyimidazole; Trypanosoma cruzi; Chagas disease; trypanocidal activity 2,4,5-triaryl-N-hydroxyimidazole; Trypanosoma cruzi; Chagas disease; trypanocidal activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Share & Cite This Article

Further Mendeley | CiteULike
Export to BibTeX |
EndNote
MDPI and ACS Style

da Silva, R.B.; Loback, V.B.; Salomão, K.; de Castro, S.L.; Wardell, J.L.; Wardell, S.M.S.V.; Costa, T.E.M.M.; Penido, C.; de Henriques, M.G.M.O.; Carvalho, S.A.; da Silva, E.F.; Fraga, C.A.M. Article Synthesis and Trypanocidal Activity of Novel 2,4,5-Triaryl-N-Hydroxylimidazole Derivatives. Molecules 2013, 18, 3445-3457.

View more citation formats

Related Articles

Article Metrics

Comments

Citing Articles

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert