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

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: Plasmodium falciparum; N-(4-piperidinyl)benzamide derivative; malaria; farnesyltransferase; inhibitor 1324

Domains: Chemical Sciences; Life Sciences [q-bio]; Microbiology and Parasitology

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, 2005, 53 (10), pp.1324-1326. ⟨10.1248/cpb.53.1324⟩. ⟨mnhn-02070112⟩