Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG).

Bioorganic & Medicinal Chemistry Letters
Denise J TsagrisSimon A Osborne

Abstract

A series of trisubstituted thiazoles have been identified as potent inhibitors of Plasmodium falciparum (Pf) cGMP-dependent protein kinase (PfPKG) through template hopping from known Eimeria PKG (EtPKG) inhibitors. The thiazole series has yielded compounds with improved potency, kinase selectivity and good in vitro ADME properties. These compounds could be useful tools in the development of new anti-malarial drugs in the fight against drug resistant malaria.

Citations

Jan 5, 2021·Frontiers in Microbiology·David A BakerMaria Penzo
Dec 16, 2019·RSC Medicinal Chemistry·Shams Ul MahmoodDavid P Rotella
Nov 12, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Chantalle MoolmanLesetja J Legoabe
Dec 19, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Romain MustièreNicolas Primas
Feb 17, 2021·ACS Infectious Diseases·Lauren B ArendseIan H Gilbert
Feb 23, 2021·Frontiers in Microbiology·David RotellaPurnima Bhanot

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