Antimalarial cyclic peroxy ketals.
Antimalarial cyclic peroxy ketals.
复制标题
抗疟环状过氧缩酮。
DOI：
10.1021/jm980088f
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发表时间：
1998
影响因子：
7.3
通讯作者：
Shapiro,TA
中科院分区：
文献类型：
--
作者：
Posner,GH;O'Dowd,H;Ploypradith,P;Cumming,JN;Xie,S;Shapiro,TA
已经通过两步方案从容易获得的芳基甲基酮开始制备了超过20种新的环状过氧缩酮。使用体外抗疟数据作为优化效力的指导，结构-活性相关性导致设计和合成了7种新的过氧化物，其IC 50值为31 - 85 nM（青蒿素IC 50 = 8.4 nM）。一些SAR的推广进行了讨论。
Over 20 new, cyclic, peroxy ketals have been prepared via a two-step protocol starting with readily available aryl methyl ketones. Structure−activity correlations using in vitro antimalarial data as a guide for optimization of potency have led to the design and synthesis of seven new peroxides that have IC50values of 31−85 nM (artemisinin IC50= 8.4 nM). Some SAR generalizations are discussed.