1. Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis
- Author
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Kevin D. Read, Sabrinia D. Crouch, Juan Miguel-Siles, Stephen Thompson, Lorna MacLean, Timothy J. Miles, Franck Martin, Alain Claude-Marie Daugan, Suzanne Norval, Laste Stojanovski, Gloria Fra, John Thomas, Frederick R. C. Simeons, Sujatha Manthri, Jose M. Fiandor, César Guerrero, Myriam Ajakane, Maria Osuna-Cabello, Paul G. Wyatt, Manu De Rycker, Lorna Campbell, Claire J. MacKenzie, Ian H. Gilbert, Jennifer Riley, Yoko Shishikura, Michael G. Thomas, and Raul F. Velasco
- Subjects
Pharmacology ,0303 health sciences ,030306 microbiology ,business.industry ,Organic Chemistry ,Pharmaceutical Science ,medicine.disease ,Biochemistry ,03 medical and health sciences ,Visceral leishmaniasis ,In vivo ,Drug Discovery ,medicine ,Molecular Medicine ,Identification (biology) ,business ,030304 developmental biology - Abstract
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.
- Published
- 2020