Antimalarial Cyclic Peroxy Ketals
- 5 May 1998
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 41 (12) , 2164-2167
- https://doi.org/10.1021/jm980088f
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
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