Ohkanda J, Lockman J W, Yokoyama K, Gelb M H, Croft S L, Kendrick H, Harrell M I, Feagin J E, Blaskovich M A, Sebti S M, Hamilton A D
Department of Chemistry, Yale University, New Haven, CT 06520, USA.
Bioorg Med Chem Lett. 2001 Mar 26;11(6):761-4. doi: 10.1016/s0960-894x(01)00055-5.
Malaria continues to represent a very serious health problem in the tropics. The current methods of clinical treatment are showing deficiencies due to the increased incidence of resistance in the parasite. In the present paper we report the design, synthesis, and evaluation of potential antimalarial agents against a novel target, protein farnesyltransferase. We show that the most potent compounds are active against Plasmodium falciparum in vitro at submicromolar concentrations.
疟疾在热带地区仍然是一个非常严重的健康问题。由于寄生虫耐药性的增加，目前的临床治疗方法存在缺陷。在本文中，我们报告了针对一种新靶点——蛋白质法尼基转移酶的潜在抗疟药物的设计、合成和评估。我们表明，最有效的化合物在体外对恶性疟原虫具有亚微摩尔浓度的活性。
