Walsh John J, Coughlan David, Heneghan Nicola, Gaynor Caroline, Bell Angus
School of Pharmacy and Pharmaceutical Sciences, Panoz Institute, Trinity College Dublin, Dublin 2, Ireland.
Bioorg Med Chem Lett. 2007 Jul 1;17(13):3599-602. doi: 10.1016/j.bmcl.2007.04.054. Epub 2007 Apr 25.
Artemisinin was reduced to dihydroartemisinin and coupled to a carboxylic acid derivative of quinine via an ester linkage. This novel hybrid molecule had potent activity against the 3D7 and (drug-resistant) FcB1 strains of Plasmodium falciparum in culture. The activity was superior to that of artemisinin alone, quinine alone, or a 1:1 mixture of artemisinin and quinine.
青蒿素被还原为双氢青蒿素,并通过酯键与奎宁的羧酸衍生物偶联。这种新型杂合分子在培养物中对恶性疟原虫的3D7和(耐药)FcB1菌株具有强大的活性。其活性优于单独使用青蒿素、单独使用奎宁或青蒿素与奎宁1:1混合物的活性。