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Novel Amino-pyrazole Ureas with Potent In Vitro and In Vivo Antileishmanial Activity

Authors :
J. Mark F. Gardner
Charles E. Mowbray
Stéphanie Braillard
Paul Alan Glossop
Karl Richard Gibson
Pim-Bart Feijens
Wen Hua
Garreth L. Morgans
Alan Daniel Brown
William Speed
Yafeng Cao
James Edward John Mills
An Matheeussen
Louis Maes
Gavin A. Whitlock
Source :
Journal of medicinal chemistry
Publication Year :
2015

Abstract

Visceral leishmaniasis is a severe parasitic disease that is one of the most neglected tropical diseases. Treatment options are limited and there is an urgent need for new therapeutic agents. Following an HTS campaign and hit optimization, a novel series of amino-pyrazole ureas has been identified with potent in vitro antileishmanial activity. Furthermore, compound 26 shows high levels of in vivo efficacy (>90%) against Leishmania infantum, thus demonstrating proof of concept for this series

Details

ISSN :
15204804 and 00222623
Volume :
58
Issue :
24
Database :
OpenAIRE
Journal :
Journal of medicinal chemistry
Accession number :
edsair.doi.dedup.....562d090d37292dd2973025263f6e0f38