桥头带有二甲氨基的双环化合物的抗原虫活性
Antiprotozoal activity of bicycles featuring a dimethylamino group at their bridgehead.
作者信息
Faist Johanna, Seebacher Werner, Saf Robert, Brun Reto, Kaiser Marcel, Weis Robert
机构信息
Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstraße 1, A-8010 Graz, Austria.
Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstraße 1, A-8010 Graz, Austria.
出版信息
Bioorg Med Chem. 2016 Aug 15;24(16):3781-9. doi: 10.1016/j.bmc.2016.06.024. Epub 2016 Jun 14.
Several dimethylamino-derivatives of the new compound-class 3-azabicyclo[3.2.2]nonanes were prepared. For better comparison of activity also a few analogues of bicyclo[2.2.2]octanes and 2-azabicyclo[3.2.2]nonanes were synthesized. Their activities were examined in vitro against the multiresistant K1 strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900). A couple of the newly synthesized compounds showed promising antiprotozoal activity and selectivity. The results of the biological tests of the novel compounds were compared with the activities of already synthesized compounds and of drugs in use. Structure-activity relationships were discussed.
制备了新化合物类别3-氮杂双环[3.2.2]壬烷的几种二甲基氨基衍生物。为了更好地比较活性，还合成了双环[2.2.2]辛烷和2-氮杂双环[3.2.2]壬烷的一些类似物。在体外检测了它们对恶性疟原虫多药耐药K1株和罗德西亚布氏锥虫（STIB 900）的活性。几种新合成的化合物显示出有前景的抗原虫活性和选择性。将这些新化合物的生物学测试结果与已合成化合物及正在使用的药物的活性进行了比较。讨论了构效关系。
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