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

A Ryckebusch; Pauline Gilleron; R Millet; R Houssin; A Lemoine; N Pommery; Philippe Grellier; C Sergheraert; J-P Henichart

doi:10.1248/cpb.53.1324

Journal articles

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

Document type :

Journal articles

Domain :

Chemical Sciences

Life Sciences [q-bio] / Microbiology and Parasitology

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Submitted on : Saturday, March 16, 2019 - 5:58:21 PM
Last modification on : Friday, December 18, 2020 - 4:31:17 PM
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Novel N-(4-Piperidinyl)benzamide Antimalarials with Mammalian Protein Farnesyltransferase Inhibitory Activity

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

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