Schlapper Christian, Seebacher Werner, Kaiser Marcel, Brun Reto, Saf Robert, Weis Robert
Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl-Franzens-University, Universitätsplatz 1, A-8010 Graz, Austria.
Bioorg Med Chem. 2007 Aug 15;15(16):5543-50. doi: 10.1016/j.bmc.2007.05.042. Epub 2007 May 23.
A couple of bicyclo[2.2.2]octyl esters of 2-dialkylaminoacetic acids were prepared. Their antiplasmodial and antitrypanosomal activities against Trypanosoma brucei rhodesiense (STIB 900) and the K(1) strain of Plasmodium falciparum (resistant to chloroquine and pyrimethamine) were determined using microplate assays. Structure-activity relationships were discussed. The antiprotozoal activities were remarkably increased by insertion of a second basic centre. The selectivity indices of the most active compounds are superior in the bicyclo-octane series.
制备了几种2-二烷基氨基乙酸的双环[2.2.2]辛酯。使用微孔板分析法测定了它们对布氏罗得西亚锥虫（STIB 900）和恶性疟原虫K(1)株（对氯喹和乙胺嘧啶耐药）的抗疟原虫和抗锥虫活性。讨论了构效关系。通过引入第二个碱性中心，抗原生动物活性显著提高。在双环辛烷系列中，活性最高的化合物的选择性指数更高。
