Novel N-(4-Piperidinyl)benzamide antimalarials with mammalian protein farnesyltransferase inhibitory activity |
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| Authors: | Ryckebusch Adina Gilleron Pauline Millet Régis Houssin Raymond Lemoine Amélie Pommery Nicole Grellier Philippe Sergheraert Christian Hénichart Jean-Pierre |
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| Institution: | Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, Université de Lille 2, France. |
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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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