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Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis.

Michael G ThomasManu De RyckerMyriam AjakaneSabrinia D CrouchLorna CampbellAlain DauganGloria FraCésar GuerreroClaire J MackenzieLorna MacLeanSujatha ManthriFranck MartinSuzanne NorvalMaria Osuna-CabelloJennifer RileyYoko ShishikuraJuan Miguel-SilesFrederick R C SimeonsLaste StojanovskiJohn ThomasStephen ThompsonRaul F VelascoJose M FiandorPaul G WyattKevin D ReadIan H GilbertTimothy J Miles
Published in: RSC medicinal chemistry (2020)
Visceral leishmaniasis (VL) affects millions of people across the world, largely in developing nations. It is fatal if left untreated and the current treatments are inadequate. As such, there is an urgent need for new, improved medicines. In this paper, we describe the identification of a 6-amino-N-(piperidin-4-yl)-1H-pyrazolo[3,4-d]pyrimidine scaffold and its optimization to give compounds which showed efficacy when orally dosed in a mouse model of VL.
Keyphrases
  • mouse model
  • bioinformatics analysis