Blumbergs P, Ao M S, LaMontagne M P, Markovac A
J Med Chem. 1975 Nov;18(11):1122-6. doi: 10.1021/jm00245a015.
Based on the high antilalarial activity of alpha-(2-piperidyl)-2,8-bis(trifluoromethyl)-4-quinolinemethanol, ten additional 2,8-bis(trifluoromethyl)-4-quinolinemethanols were prepared in which the amino alcohol side chain was structurally varied. Synthesis of the compounds is described and antimalarial activity data against Plasmodium berghei are presented and discussed in terms of the structure variations.
基于α-(2-哌啶基)-2,8-双(三氟甲基)-4-喹啉甲醇的高抗疟活性,制备了另外十种2,8-双(三氟甲基)-4-喹啉甲醇,其中氨基醇侧链在结构上有所变化。描述了这些化合物的合成过程,并根据结构变化给出并讨论了针对伯氏疟原虫的抗疟活性数据。