Dutta G P, Puri S K, Bhaduri A P, Seth M
Division of Microbiology and Medicinal Chemistry, Central Drug Research Institute, Lucknow, India.
Am J Trop Med Hyg. 1989 Dec;41(6):635-7. doi: 10.4269/ajtmh.1989.41.635.
An analogue of primaquine, N1-(3-acetyl-4-5-dihydro-2-furanyl)-N4-(6-methoxy-8-quinolinyl) 1,4-pentanediamine, CDRI Code 80/53), has been evaluated for anti-relapse activity against sporozoite induced Plasmodium cynomolgi B infection in rhesus monkeys. The compound has shown 100% curative anti-relapse activity at 1.25 mg/kg x 7 day dose schedule, thereby giving a primaquine index of 0.8. The compound is currently under Phase-I clinical trials.
伯氨喹的类似物,N1-(3-乙酰基-4,5-二氢-2-呋喃基)-N4-(6-甲氧基-8-喹啉基)1,4-戊二胺,CDRI编码80/53,已针对食蟹猴疟原虫B感染恒河猴时子孢子诱导的复发活性进行了评估。该化合物在1.25mg/kg×7天的剂量方案下显示出100%的抗复发治愈活性,因此伯氨喹指数为0.8。该化合物目前正处于I期临床试验阶段。