Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Notes
Novel N-(4-Piperidinyl)benzamide Antimalarials with Mammalian Protein Farnesyltransferase Inhibitory Activity
Adina RyckebuschPauline GilleronRégis MilletRaymond HoussinAmélie LemoineNicole PommeryPhilippe GrellierChristian SergheraertJean-Pierre Hénichart
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2005 Volume 53 Issue 10 Pages 1324-1326

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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.

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© 2005 The Pharmaceutical Society of Japan
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