Design, synthesis and antimalarial activity of novel, quinoline-based, zinc metallo-aminopeptidase inhibitors

…, P Grellier, C Sergheraert, R Deprez-Poulain

文献索引：Flipo, Marian; Florent, Isabelle; Grellier, Philippe; Sergheraert, Christian; Deprez-Poulain, Rebecca Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 16 p. 2659 - 2662

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被引用次数: 44

摘要

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 IC50 of 854 nM. The antimalarial activity on a CQ-resistant strain and the specificity towards mammalian aminopeptidase N are also discussed.