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Novel N-(4-Piperidinyl)benzamide Antimalarials with Mammalian Protein Farnesyltransferase Inhibitory Activity

A Ryckebusch 1 Pauline Gilleron 1 R Millet 1 R Houssin 1 A Lemoine 1 N Pommery 1 Philippe Grellier 2 C Sergheraert 3 J-P Henichart 1
1 ICPAL - Institut de Chimie Pharmaceutique Albert Lespagnol
2 MCAM - Molécules de Communication et Adaptation des Micro-organismes
3 SSFB - Synthèse, structure et fonction des biomolécules
Abstract : Protein farnesyltransferase of Plasmodium falciparum is a potential target in the treatment of malaria for which increased drug resistance is observed. The design, synthesis and evaluation of a series of N-(4-piperidinyl)benzamides is reported. The most potent compounds showed in vitro activity against the parasite at submicromolar concentrations.
Keywords : inhibitor 1324 farnesyltransferase malaria Plasmodium falciparum N-(4-piperidinyl)benzamide derivative
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A Ryckebusch, Pauline Gilleron, R Millet, R Houssin, A Lemoine, et al.. Novel N-(4-Piperidinyl)benzamide Antimalarials with Mammalian Protein Farnesyltransferase Inhibitory Activity. Chemical and Pharmaceutical Bulletin, Pharmaceutical Society of Japan, 2005, 53 (10), pp.1324-1326. ⟨10.1248/cpb.53.1324⟩. ⟨mnhn-02070112⟩

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