Antimalarial cyclic peroxy ketals |
| |
| Authors: | GH Posner H O'Dowd P Ploypradith JN Cumming S Xie TA Shapiro |
| |
| Affiliation: | Department of Chemistry, The Johns Hopkins University, Baltimore, Maryland 21218, USA. |
| |
| Abstract: | 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 IC50 values of 31-85 nM (artemisinin IC50 = 8.4 nM). Some SAR generalizations are discussed. |
| |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ |
|
