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ID: ALA1136149
Journal: Bioorg Med Chem Lett
Title: Design, synthesis and antimalarial activity of novel, quinoline-based, zinc metallo-aminopeptidase inhibitors.
Authors: Flipo M, Florent I, Grellier P, Sergheraert C, Deprez-Poulain R.
Abstract: PfA-M1, a neutral zinc aminopeptidase of Plasmodium falciparum, is a new potential target for the discovery of antimalarials. The design and synthesis of a library of 45 quinoline-based inhibitors of PfA-M1 is reported. The best inhibitor displays an IC(50) of 854 nM. The antimalarial activity on a CQ-resistant strain and the specificity towards mammalian aminopeptidase N are also discussed.
CiteXplore: 12873488