Antimalarial Cyclic Peroxy Ketals

Autor: Posner, G. H., O'Dowd, H., Ploypradith, P., Cumming, J. N., Xie, S., Shapiro, T. A.
Zdroj: Journal of Medicinal Chemistry; June 4, 1998, Vol. 41 Issue: 12 p2164-2167, 4p
Abstrakt: 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.
Databáze: Supplemental Index