Instituto de Tecnologia em Fármacos-Farmanguinhos, FioCruz-Fundacao Oswaldo Cruz, R. Sizenando Nabuco, 100, Manguinhos, 21041-250, Rio de Janeiro, RJ, Brazil.
Med Chem. 2012 Mar;8(2):266-72. doi: 10.2174/157340612800493638.
A series of hydroxyethylamines has been synthesized from the reaction of (2S,3S )Boc-phenylalanine epoxide with alkyl amines in good yields and evaluated for their in vivo antimalarial activity in mice. Compound 4g presented better activity then the reference artesunate in percentage of inhibition of parasitemia in treated P. berghei-infected mice and compare to the activity of artesunate in the survival of mice 14 days after infection. In addiction, no hemolytic activity was found, which supports that inhibition of parasitemia is due to antimalarial activity. The compound 4g inhibited the differentiation to schizonts suggesting that parasite metabolism is a possible target of 4g. These results indicate that this class of compound possesses promising perspectives for the development of new antimalarial drugs.
已经从（2S,3S ）Boc-苯丙氨酸环氧化物与烷基胺的反应中合成了一系列羟乙胺，并对其在体内的抗疟活性进行了评估。化合物 4g 在治疗感染 P. berghei 的小鼠体内疟原虫抑制率方面比参考药物青蒿琥酯具有更好的活性，并且与感染后 14 天青蒿琥酯在小鼠存活率方面的活性相比也具有更好的活性。此外，没有发现溶血活性，这表明抑制疟原虫是由于抗疟活性。化合物 4g 抑制了裂殖体的分化，这表明寄生虫的代谢可能是 4g 的一个潜在靶点。这些结果表明，这类化合物具有开发新型抗疟药物的广阔前景。
