Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 58, Issue 24, Pages 9615-9624Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b01456
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Funding
- United Kingdom Department for International Development (DFID)
- Dutch Ministry of Foreign Affairs (DGIS)
- Swiss Agency for Development and Cooperation (SDC)
- Bill & Melinda Gates Foundation
- German Federal Ministry of Education and Research (BMBF) through KfW
- Medecins Sans Frontieres (Doctors without Borders)
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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, 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.
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