jm980088f_si_001.pdf (421.59 kB)
Antimalarial Cyclic Peroxy Ketals
journal contribution
posted on 1998-05-05, 00:00 authored by Gary H. Posner, Hardwin O'Dowd, Poonsakdi Ploypradith, Jared N. Cumming, Suji Xie, Theresa A. ShapiroOver 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.