Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivoefficacy against visceral leishmaniasisElectronic supplementary information (ESI) available. See DOI: 10.1039/d0md00203h

Autor: Thomas, Michael G., De Rycker, Manu, Ajakane, Myriam, Crouch, Sabrinia D., Campbell, Lorna, Daugan, Alain, Fra, Gloria, Guerrero, César, Mackenzie, Claire J., MacLean, Lorna, Manthri, Sujatha, Martin, Franck, Norval, Suzanne, Osuna-Cabello, Maria, Riley, Jennifer, Shishikura, Yoko, Miguel-Siles, Juan, Simeons, Frederick R. C., Stojanovski, Laste, Thomas, John, Thompson, Stephen, Velasco, Raul F., Fiandor, Jose M., Wyatt, Paul G., Read, Kevin D., Gilbert, Ian H., Miles, Timothy J.
Zdroj: MedChemComm; 2020, Vol. 11 Issue: 10 p1168-1177, 10p
Abstrakt: 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.
Databáze: Supplemental Index