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

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• 作者：Charles E. Mowbray ; Stéphanie Braillard ; William Speed ; Paul A. Glossop ; Gavin A. Whitlock ; Karl R. Gibson ; James E. J. Mills ; Alan D. Brown ; J. Mark F. Gardner ; Yafeng Cao ; Wen Hua ; Garreth L. Morgans ; Pim-Bart Feijens ; An Matheeussen ; Louis J. Maes
• 刊名：Journal of Medicinal Chemistry
• 出版年：2015
• 出版时间：December 24, 2015
• 年：2015
• 卷：58
• 期：24
• 页码：9615-9624
• 全文大小：376K
• ISSN：1520-4804

文摘

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.