Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids

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• 作者：Johanna Faist ; Werner Seebacher ; Christian Schlapper ; Marcel Kaiser ; Reto Brun ; Robert Saf ; Robert Weis
• 关键词：Amino acids ; 4-Aminobicyclo-octanes ; 5-Amino-2-azabicyclo-nonanes ; Plasmodium berghei ; Plasmodium falciparum ; Trypanosoma brucei rhodesiense
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2009
• 出版时间：15 May 2009
• 年：2009
• 卷：17
• 期：10
• 页码：3595-3603
• 全文大小：267 K

文摘

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.