Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitätsplatz 1, A-8010 Graz, Austria.
Bioorg Med Chem. 2010 Sep 15;18(18):6796-804. doi: 10.1016/j.bmc.2010.07.046. Epub 2010 Jul 25.
Dialkylaminoalkyl derivatives of 2-azabicyclo[3.2.2]nonanes and of bicyclo[2.2.2]octanes were prepared and their activities determined in vitro against the multiresistant K1 strain of Plasmodium falciparum. Several of the new compounds exhibited very promising antiplasmodial activity and selectivity. The results were compared to those of formerly synthesized analogues and of drugs in use. Structure-activity relationships were detected. Some of the more potent compounds were tested in vivo against Plasmodium berghei showing weak to moderate activity. A single compound was able to increase the mean survival days of infected mice.
合成了 2-氮杂双环[3.2.2]壬烷和双环[2.2.2]辛烷的二烷基氨基烷基衍生物，并在体外对耐多药恶性疟原虫 K1 株进行了活性测定。一些新化合物表现出非常有前途的抗疟活性和选择性。结果与以前合成的类似物和现有的药物进行了比较。检测到了结构-活性关系。一些效力更强的化合物在体内对伯氏疟原虫进行了测试，显示出弱至中等的活性。一种单一的化合物能够延长感染小鼠的平均存活天数。
