二烷基氨基酸的双环酰胺和酯的抗疟原虫及抗锥虫活性
Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids.
作者信息
Faist Johanna, Seebacher Werner, Schlapper Christian, Kaiser Marcel, Brun Reto, Saf Robert, Weis Robert
机构信息
Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitätsplatz 1, A-8010 Graz, Austria.
出版信息
Bioorg Med Chem. 2009 May 15;17(10):3595-603. doi: 10.1016/j.bmc.2009.04.002. Epub 2009 Apr 7.
Several bicyclic amides and esters of dialkylamino acids were prepared. Their activities against a multiresistant strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900) were examined. Structure-activity relationships were discussed. Particularly the ester compounds showed good antiplasmodial and antitrypanosomal activity and a single compound was tested in vivo against Plasmodium berghei.
制备了几种二烷基氨基酸的双环酰胺和酯。检测了它们对恶性疟原虫多抗性菌株以及罗德西亚布氏锥虫（STIB 900）的活性。讨论了构效关系。特别是酯类化合物显示出良好的抗疟和抗锥虫活性，并且对一种化合物进行了体内抗伯氏疟原虫试验。
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