Antimalarial cyclic peroxy ketals.

G H Posner; H O'Dowd; P Ploypradith; J N Cumming; S Xie; T A Shapiro

doi:10.1021/jm980088f

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Antimalarial cyclic peroxy ketals.

G H Posner·H O'Dowd·P Ploypradith·J N Cumming·S Xie·T A Shapiro

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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.

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Animals Antimalarials Artemisinins Drug Design Heterocyclic Compounds Plasmodium falciparum Sesquiterpenes Structure-Activity Relationship Journal Article Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, P.H.S.

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G H Posner, H O'Dowd, P Ploypradith, J N Cumming, S Xie, T A Shapiro. 1998-06-04. Antimalarial cyclic peroxy ketals.. https://doi.org/10.1021/jm980088f

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