Discovery of pyridyl-based inhibitors of Plasmodium falciparum N -myristoyltransferase.
MEDCHEMCOMM(2015)
摘要
-Myristoyltransferase (NMT) represents an attractive drug target in parasitic infections such as malaria due to its genetic essentiality and amenability to inhibition by drug-like small molecules. Scaffold simplification from previously reported inhibitors containing bicyclic cores identified phenyl derivative , providing a versatile platform to study the effects of substitution on the scaffold, which yielded pyridyl . This molecule exhibited improved enzyme and cellular potency, and reduced lipophilicity compared to inhibitor . Further structure-based inhibitor design led to the discovery of , the most potent inhibitor in this series, which showed single-digit nM enzyme affinity and sub-μM anti-plasmodial activity.
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关键词
inhibitors,pyridyl-based,n-myristoyltransferase
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