Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7

N Bouloc, JM Large, E Smiljanic, D Whalley…

Index: Bouloc, Nathalie; Large, Jonathan M.; Smiljanic, Ela; Whalley, David; Ansell, Keith H.; Edlin, Christopher D.; Bryans, Justin S. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 19 p. 5294 - 5298

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Citation Number: 32

Abstract

A high-throughput screening campaign identified a number of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7. Further synthetic chemistry efforts enabled the preparation of a number of analogues with promising in vitro potencies. Although these compounds show likely broad spectrum inhibitory activity, they represent a useful starting point for further chemical optimisation.