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Development of Simplified Heterocyclic Acetogenin Analogues as Potent and SelectiveTrypanosoma bruceiInhibitors

Authors :
Terry K. Smith
Marija K. Zacharova
Gordon J. Florence
Stefanie K. Menzies
Lindsay B. Tulloch
Marie I. Thomson
Andrew L. Fraser
Elizabeth F. B. King
Joanne C. Morris
Eoin R. Gould
Source :
Chemmedchem
Publication Year :
2016
Publisher :
Wiley, 2016.

Abstract

Neglected tropical diseases caused by parasitic infections are an ongoing and increasing concern. They are a burden to human and animal health, having the most devastating effect on the world′s poorest countries. Building upon our previously reported triazole analogues, in this study we describe the synthesis and biological testing of other novel heterocyclic acetogenin‐inspired derivatives, namely 3,5‐isoxazoles, furoxans, and furazans. Several of these compounds maintain low‐micromolar levels of inhibition against Trypanosoma brucei, whilst having no observable inhibitory effect on mammalian cells, leading to the possibility of novel lead compounds for selective treatment.

Details

ISSN :
18607179
Volume :
11
Database :
OpenAIRE
Journal :
ChemMedChem
Accession number :
edsair.doi.dedup.....2f8e6f1d792dd488a2bb5f1e4565e36c
Full Text :
https://doi.org/10.1002/cmdc.201600210