ANTIMALARIAL CYCLIC PEROXY KETALS

Authors
POSNER GH ODOWD H PLOYPRADITH P CUMMING JN XIE S SHAPIRO TA
Citation
Gh. Posner et al., ANTIMALARIAL CYCLIC PEROXY KETALS, Journal of medicinal chemistry, 41(12), 1998, pp. 2164-2167
Citations number
26
Categorie Soggetti
Chemistry Medicinal
Journal title
Journal of medicinal chemistry → ACNP
ISSN journal
00222623
Volume
41
Issue
12
Year of publication
1998
Pages
2164 - 2167
Database
ISI
SICI code
0022-2623(1998)41:12<2164:ACPK>2.0.ZU;2-F
Abstract
Over 20 new, cyclic, peroxy ketals have been prepared via a two-step p rotocol 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.