Department of Pharmaceutical Chemistry, North-West University, Potchefstroom, South Africa.
Bioorg Med Chem Lett. 2010 Dec 1;20(23):6975-7. doi: 10.1016/j.bmcl.2010.09.130. Epub 2010 Oct 21.
Novel artemisinin-quinoline hybrid-dimers were synthesized from dihydroartemisinin and different aminoquinolines at elevated temperatures (90-110°C). All compounds were obtained as the β-isomers and were tested against both chloroquine sensitive and resistant strains of Plasmodium falciparum. Hybrid-dimer 8 showed the highest antiplasmodial activity, inheriting the optimum chain length of three carbon atoms.
新型青蒿素-喹啉杂二聚体由二氢青蒿素和不同的氨基喹啉在高温(90-110°C)下合成。所有化合物均以β-异构体获得,并对氯喹敏感和耐药的恶性疟原虫株进行了测试。杂二聚体 8 表现出最高的抗疟活性,继承了最佳的三个碳原子链长。