Publication | Closed Access
Novel Amino-pyrazole Ureas with Potent In Vitro and In Vivo Antileishmanial Activity
66
Citations
31
References
2015
Year
Medicinal ChemistryVivo Antileishmanial ActivityBioorganic ChemistryPharmaceutical ChemistryBiochemistryAntiparasitic AgentLeishmania InfantumNatural SciencesMedicineParasitic ProtozoaAntifungal AgentVitro Antileishmanial ActivityDrug DevelopmentPharmacologyVisceral LeishmaniasisNovel Amino-pyrazole UreasDrug DiscoveryDrug Resistance
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.
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