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抗疟药。12. 作为抑制性抗疟药的选定4-吡啶甲醇的碳等排体的制备。

Antimalarials. 12. Preparation of carbon isosteres of selected 4-pyridinemethanols as suppressive antimalarials.

作者信息

Markovac A, LaMontagne M P

出版信息

J Med Chem. 1980 Nov;23(11):1198-201. doi: 10.1021/jm00185a009.

Abstract

Four carbon isosteres related to the highly active 4-pyridylcarbinolamines were prepared and evaluated for suppressive antimalarial activity against Plasmodium berghei in mice. Three of the four examples possessed significant activity but were approximately one dose level less active than the corresponding pyridines.

摘要

制备了与高活性4-吡啶甲醇胺相关的四种碳等排体,并评估了它们对小鼠伯氏疟原虫的抑制抗疟活性。四个实例中的三个具有显著活性,但活性比相应的吡啶低约一个剂量水平。

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