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

Abstract : PfA-M1, a neutral zinc aminopeptidase of Plasmodium falciparum, is a new potential target for the discovery of anti-malarials. 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. #
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https://hal-mnhn.archives-ouvertes.fr/mnhn-02867485
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Marian Flipo, Isabelle Florent, Philippe Grellier, Christian Sergheraert, Rebecca Déprez-Poulain. Design, synthesis and antimalarial activity of novel, quinoline-Based, zinc metallo-aminopeptidase inhibitors. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2003, 13 (16), pp.2659-2662. ⟨10.1016/S0960-894X(03)00550-X⟩. ⟨mnhn-02867485⟩

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