Issue 10, 2020

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

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.

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

Supplementary files

Article information

Article type
Research Article
Submitted
12 Jun 2020
Accepted
07 Jul 2020
First published
06 Aug 2020
This article is Open Access
Creative Commons BY license

RSC Med. Chem., 2020,11, 1168-1177

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

M. G. Thomas, M. De Rycker, M. Ajakane, S. D. Crouch, L. Campbell, A. Daugan, G. Fra, C. Guerrero, C. J. Mackenzie, L. MacLean, S. Manthri, F. Martin, S. Norval, M. Osuna-Cabello, J. Riley, Y. Shishikura, J. Miguel-Siles, F. R. C. Simeons, L. Stojanovski, J. Thomas, S. Thompson, R. F. Velasco, J. M. Fiandor, P. G. Wyatt, K. D. Read, I. H. Gilbert and T. J. Miles, RSC Med. Chem., 2020, 11, 1168 DOI: 10.1039/D0MD00203H

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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