3-氮杂双环[3.2.2]壬烷的合成及其抗寄生虫活性。
Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities.
作者信息
Seebacher Werner, Wolkinger Volker, Faist Johanna, Kaiser Marcel, Brun Reto, Saf Robert, Bucar Franz, Gröblacher Barbara, Brantner Adelheid, Merino Virginia, Kalia Yogeshvar, Scapozza Leonardo, Perozzo Remo, Weis Robert
机构信息
Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl-Franzens-University, Schubertstrasse 1, Graz A-8010, Austria.
Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl-Franzens-University, Schubertstrasse 1, Graz A-8010, Austria.
出版信息
Bioorg Med Chem Lett. 2015 Apr 1;25(7):1390-3. doi: 10.1016/j.bmcl.2015.02.044. Epub 2015 Feb 28.
Several bicyclic compounds, 3-azabicyclo[3.2.2]nonanes, have been prepared. The new compounds were tested for their activities against one strain of the causative organism of Malaria tropica, Plasmodium falciparum K1, which is resistant against chloroquine and pyrimethamine. In addition, their cytotoxicity and their activity against the pathogen of the East African form of sleeping sickness, Trypanosoma brucei rhodesiense, were investigated. Structure-activity relationships are discussed considering data of readily prepared compounds. For the first time, a distinct in vivo activity was observed against Plasmodium berghei in a mouse model. The active compound was further investigated.
已经制备了几种双环化合物，即3-氮杂双环[3.2.2]壬烷。测试了这些新化合物对热带疟原虫（Plasmodium falciparum K1）这一致病生物体菌株的活性，该菌株对氯喹和乙胺嘧啶具有抗性。此外，还研究了它们的细胞毒性以及对东非昏睡病病原体布氏罗得西亚锥虫（Trypanosoma brucei rhodesiense）的活性。结合易于制备的化合物的数据讨论了构效关系。首次在小鼠模型中观察到对伯氏疟原虫（Plasmodium berghei）有明显的体内活性。对活性化合物进行了进一步研究。
Zotero 插件