Ryckebusch Adina, Gilleron Pauline, Millet Régis, Houssin Raymond, Lemoine Amélie, Pommery Nicole, Grellier Philippe, Sergheraert Christian, Hénichart Jean-Pierre
Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, Université de Lille 2, France.
Chem Pharm Bull (Tokyo). 2005 Oct;53(10):1324-6. doi: 10.1248/cpb.53.1324.
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.
恶性疟原虫的蛋白质法尼基转移酶是疟疾治疗中的一个潜在靶点，目前已观察到针对该靶点的耐药性增加。本文报道了一系列N-(4-哌啶基)苯甲酰胺的设计、合成及评估。最具活性的化合物在亚微摩尔浓度下对该寄生虫表现出体外活性。
