4-Aminobicyclo[2.2.2]octanone Derivatives with Antiprotozoal Activities
4-Aminobicyclo[2.2.2]octanone Derivatives with Antiprotozoal Activities
复制标题
具有抗原虫活性的4-氨基双环[2.2.2]辛酮衍生物
DOI：
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发表时间：
2003
期刊：
影响因子：
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通讯作者：
W. Seebacher
中科院分区：
文献类型：
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作者：
R. Weis;R. Brun;R. Saf;W. Seebacher
概述.在一锅反应中由亚苄基丙酮和硫氰酸二烷基铵制备的4-氨基双环[2.2.2]辛酮被立体选择性地还原成它们相应的醇。 研究了双环化合物对热带疾病病原生物的活性。4-氨基双环[2.2.2]辛-2-醇通常对锥虫B具有更高的活性。与相应的酮化合物相比，Rhodesiense和恶性疟原虫的活性更高。
Summary. 4-Aminobicyclo[2.2.2]octanones which were prepared in one-pot-reactions from benzylidene acetone and dialkylammonium rhodanides were reduced stereoselectively to their corresponding alcohols. The activities of the bicyclic compounds against causative organisms of tropical deseases were examined. The 4-aminobicyclo[2.2.2]octan-2-ols were in general more active against Trypanosoma b. rhodesiense and Plasmodium falciparum than the corresponding keto compounds.