青蒿素是当前治疗抗恶性疟疾的首选药物。为克服它的近期复燃率高的缺点,我们以还原青蒿素为中间体,在酸或碱的催化下与各种醇、羧酸酐或酰氯、氯甲酸酯反应,合成了它的醚类,羧酸酯类和碳酸酯类衍生物47个。经鼠疟(P.berghei)抗氯喹原虫株筛选,发现其中大多数化合物的抗疟效果超过青蒿素;以SD_(90)作比较标准,超过青蒿素十倍左右的化合物有12个。 Artemisinin is currently the drug of choice for treating falciparum malaria. In order to overcome its shortcomings of high re-ignition rate, we have synthesized the ether by using artemisinin as the intermediate to react with various alcohols, carboxylic anhydrides or acid chlorides and chloroformates under the catalysis of acids or bases. There are 47 carboxylic acid esters and carbonate derivatives. Through the screening of P. berghei against chloroquine strains, the antimalarial effect of most of the compounds was found to be superior to artemisinin; with SD_(90) as the comparison standard, there were 12 compounds that were approximately ten times more than artemisinin.