Hamer M, Batzer O F, Moats M J, Wu C C, Lira E P
J Pharm Sci. 1975 Dec;64(12):1961-4. doi: 10.1002/jps.2600641211.
A series of substituted 2-pyridyl-alpha-toluenesulfonates was synthesized for antimalarial testing. They were prepared by treating various 2-pyridinols with alpha-toluenesulfonyl chlorides in the presence of an alkali. In tests against Plasmodium berghei in mice at 640 mg/kg, only 3,5-dichloro-2-pyridyl-alpha-toluenesulfonate was considered active, i.e., doubled the mean survival time.
合成了一系列取代的2-吡啶基-α-甲苯磺酸盐用于抗疟测试。它们是通过在碱存在下用α-甲苯磺酰氯处理各种2-吡啶醇制备的。在对小鼠体内伯氏疟原虫的测试中，剂量为640mg/kg时，只有3,5-二氯-2-吡啶基-α-甲苯磺酸盐被认为具有活性，即平均存活时间延长了一倍。
