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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.

SUBMITTER: Thomas MG

PROVIDER: S-EPMC7651859 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature

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

Thomas Michael G MG De Rycker Manu M Ajakane Myriam M Crouch Sabrinia D SD Campbell Lorna L Daugan Alain A Fra Gloria G Guerrero César C Mackenzie Claire J CJ MacLean Lorna L Manthri Sujatha S Martin Franck F Norval Suzanne S Osuna-Cabello Maria M Riley Jennifer J Shishikura Yoko Y Miguel-Siles Juan J Simeons Frederick R C FRC Stojanovski Laste L Thomas John J Thompson Stephen S Velasco Raul F RF Fiandor Jose M JM Wyatt Paul G PG Read Kevin D KD Gilbert Ian H IH Miles Timothy J TJ

RSC medicinal chemistry 20200806 10

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. ...[more]

PMID: 33479621

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