Trisubstituted Thiazoles As Potent and Selective Inhibitors of Plasmodium Falciparum Protein Kinase G (PfPKG)

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2018 Sep 4

PMID 30174152

Citations 16

Authors

Denise J Tsagris

Kristian Birchall

Nathalie Bouloc

Jonathan M Large

Andy Merritt

Ela Smiljanic-Hurley

Mary Wheldon

Keith H Ansell

Catherine Kettleborough

David Whalley

Lindsay B Stewart

Paul W Bowyer

David A Baker

Simon A Osborne

Affiliations

Soon will be listed here.

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.

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