Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity

J Ohkanda, JW Lockman, K Yokoyama, MH Gelb…

文献索引：Ohkanda, Junko; Lockman, Jeffrey W.; Yokoyama, Kohei; Gelb, Michael H.; Croft, Simon L.; Kendrick, Howard; Harrell, Maria Isabel; Feagin, Jean E.; Blaskovich, Michelle A.; Sebti, Said M.; Hamilton, Andrew D. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 6 p. 761 - 764

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被引用次数: 86

摘要

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 ...