Hochegger Patrick, Faist Johanna, Seebacher Werner, Saf Robert, Mäser Pascal, Kaiser Marcel, Weis Robert
Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstraße 1, A-8010 Graz, Austria.
Institute for Chemistry and Technology of Materials (ICTM), University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
Bioorg Med Chem. 2017 Apr 1;25(7):2251-2259. doi: 10.1016/j.bmc.2017.02.043. Epub 2017 Feb 24.
New analogues of the recently published compound DDD107498 were prepared. Their activities were examined in vitro against the chloroquine-sensitive NF54 strain. The most active were also tested against the multiresistant K strain of Plasmodium falciparum. A couple of the newly synthesized compounds showed promising antiplasmodial activity and selectivity. A single compound showed adequate reduction of parasitaemia (98.1%) in mice infected with Plasmodium berghei. Survival time was doubled compared to control. The results of the biological tests of the novel compounds were compared with the activities of drugs in use. Structure-activity relationships were discussed.
制备了最近发表的化合物DDD107498的新类似物。在体外检测了它们对氯喹敏感的NF54菌株的活性。还对活性最高的化合物针对恶性疟原虫的多抗性K菌株进行了测试。几种新合成的化合物显示出有前景的抗疟活性和选择性。一种单一化合物在感染伯氏疟原虫的小鼠中显示出足够的寄生虫血症降低率（98.1%）。与对照组相比，存活时间延长了一倍。将这些新化合物的生物学测试结果与现有药物的活性进行了比较。讨论了构效关系。
