Markovac A, LaMontagne M P
J Med Chem. 1976 Jul;19(7):978-82. doi: 10.1021/jm00229a027.
Nine di- and trisubstituted 9-phenanthrenemethanols bearing methylthio and methylfulfonyl substituents in the 2 and/or 6 positions of the phenanthrene nucleus were prepared and screened for antimalarial activity against Plasmodium berghei in mice. Six of the nine compounds were curative at or below 160 mg/kg. The most active structures contained a methylthio substituent in combination with two chlorine atoms.
制备了九种在菲核的2位和/或6位带有甲硫基和甲基磺酰基取代基的二取代和三取代9-菲甲醇,并针对小鼠体内的伯氏疟原虫进行了抗疟活性筛选。这九种化合物中有六种在160mg/kg及以下剂量时具有治愈效果。活性最高的结构含有一个甲硫基取代基以及两个氯原子。