Novel N-(4-piperidinyl) benzamide antimalarials with mammalian protein farnesyltransferase inhibitory activity
A Ryckebusch, P Gilleron, R Millet, R Houssin…
Index: Ryckebusch, Adina; Gilleron, Pauline; Millet, Regis; Houssin, Raymond; Lemoine, Amelie; Pommery, Nicole; Grellier, Philippe; Sergheraert, Christian; Henichart, Jean-Pierre Chemical and Pharmaceutical Bulletin, 2005 , vol. 53, # 10 p. 1324 - 1326
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Citation Number: 13
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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