3-羟烷基-2-亚甲基丙酸衍生物的抗疟活性
Antimalarial activity of 3-hydroxyalkyl-2-methylene-propionic acid derivatives.
作者信息
Kundu M K, Kundu M K, Sundar N, Kumar S K, Bhat S V, Biswas S, Valecha N
机构信息
Department of Chemistry, Indian Institute of Technology, Powai, Bombay.
出版信息
Bioorg Med Chem Lett. 1999 Mar 8;9(5):731-6. doi: 10.1016/s0960-894x(99)00057-8.
Abstract
Several Baylis-Hillman adducts and their derivatives were synthesized and evaluated as targeted potential anti-malarials. The compounds 4, 7 and 9 were found to have highest potency against P. falciparum in vitro. The in vivo test result of compound 4 and 9 against P. berghei demonstrated activity at 80 mg/Kg dose level.
摘要
合成了几种贝利斯-希尔曼加合物及其衍生物，并将其作为潜在的靶向抗疟药物进行评估。发现化合物4、7和9在体外对恶性疟原虫具有最高的效力。化合物4和9对伯氏疟原虫的体内试验结果表明，在80mg/Kg剂量水平具有活性。
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