Design and synthesis of inhibitors of Plasmodium falciparum N-myristoyltransferase, a promising target for anti-malarial drug discovery


Design of inhibitors for N-myristoyltransferase (NMT), an enzyme responsible for protein trafficking in Plasmodium falciparum , the most lethal species of parasites that cause malaria, is described. Chemistry-driven optimization of compound 1 from a focused NMT inhibitor library led to the identification of two early lead compounds 4 and 25, which showed good enzyme and cellular potency and excellent selectivity over human NMT. These molecules provide a valuable starting point for further development.

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Volume 55
Issue number 20
Pages 8879-8890
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