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

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-...

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Detalles Bibliográficos
Autores principales: 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.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Royal Society of Chemistry 2020
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7651859/
https://www.ncbi.nlm.nih.gov/pubmed/33479621
http://dx.doi.org/10.1039/d0md00203h
Descripción
Sumario: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.

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