Title of article
Design, synthesis and antimalarial activity of novel, quinoline-Based, zinc metallo-aminopeptidase inhibitors
Author/Authors
Marian Flipo، نويسنده , , Isabelle Florent، نويسنده , , Philippe Grellier، نويسنده , , Christian Sergheraert، نويسنده , , Rebecca Deprez-Poulain، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
4
From page
2659
To page
2662
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 IC50 of 854 nM. The antimalarial activity on a CQ-resistant strain and the specificity towards mammalian aminopeptidase N are also discussed.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793421
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