过氧化物作为氧化型抗疟药。
Peroxides as oxidant antimalarials.
作者信息
Vennerstrom J L, Acton N, Lin A J, Klayman D L
机构信息
Department of Medicinal Chemistry, Walter Reed Army Institute of Research, Washington, DC 20307.
出版信息
Drug Des Deliv. 1989 Jan;4(1):45-54.
To further explore the antimalarial activity of peroxides (e.g. artemisinin 1), twenty-three peroxides (all the compounds shown in Figures 3 and 4) of diverse chemical structure and acceptable stability were selected and tested for antimalarial activity in vitro against Plasmodium falciparum, and in mice against P. berghei. Included were hydroperoxides, dialkyl peroxides, acyl and diacylperoxides, peroxyketals, peroxycarbonates, and endoperoxides. None was active in vivo, although several were reasonably potent in vitro.
为了进一步探究过氧化物（如青蒿素1）的抗疟活性，我们选择了23种化学结构各异且稳定性尚可的过氧化物（图3和图4中所示的所有化合物），并对其进行体外抗恶性疟原虫活性以及在小鼠体内抗伯氏疟原虫活性的测试。这些过氧化物包括氢过氧化物、二烷基过氧化物、酰基和二酰基过氧化物、过氧化缩酮、过氧碳酸盐和内过氧化物。尽管其中几种在体外具有相当强的活性，但无一在体内具有活性。
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