Antiprotozoal activity of bicyclic diamines with a N-methylpiperazinyl group at the bridgehead atom

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• 作者：Johanna Faist ; Werner Seebacher ; Marcel Kaiser ; Reto Brun ; Robert Saf ; Robert Weis
• 关键词：4-(4-Methylpiperazin-1-yl)bicyclo[2.2.2]octanes ; 5-(4-Methylpiperazin-1-yl)-2-azabicyclo[3.2.2]nonanes ; Plasmodium falciparum ; Trypanosoma brucei rhodesiense
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2013
• 出版时间：1 September, 2013
• 年：2013
• 卷：21
• 期：17
• 页码：4988-4996
• 全文大小：674 K

文摘

¦Ø-Aminoacyl and -alkyl derivatives of 4-(4-methylpiperazin-1-yl)bicyclo[2.2.2]octan-2-amines and of 5-(4-methylpiperazin-1-yl)-2-azabicyclo[3.2.2]nonanes were prepared and their activities were examined in vitro against the multiresistant K₁ strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900). Some of the newly synthesized compounds showed very promising antiprotozoal activity and selectivity. A few of the alkylamino-2-azabicyclo[3.2.2]nonanes exhibited high antiplasmodial activity, whereas a single bicyclo[2.2.2]octane derivative was the most potent antitrypanosomal compound. The results of the newly synthesized compounds were compared with the activities of already synthesized compounds and of drugs in use. Structure-activity relationships were discussed.