Antimalarial cyclic peroxy ketals

Gary H. Posner; Hardwin O'Dowd; Poonsakdi Ploypradith; Jared N. Gumming; Suji Xie; Theresa A. Shapiro

doi:10.1021/jm980088f

Antimalarial cyclic peroxy ketals

Gary H. Posner, Hardwin O'Dowd, Poonsakdi Ploypradith, Jared N. Gumming, Suji Xie, Theresa A. Shapiro

Research output: Contribution to journal › Article › peer-review

67 Scopus citations

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 anti-malarial 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.

Original language	English (US)
Pages (from-to)	2164-2167
Number of pages	4
Journal	Journal of medicinal chemistry
Volume	41
Issue number	12
DOIs	https://doi.org/10.1021/jm980088f
State	Published - Jun 4 1998
Externally published	Yes

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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10.1021/jm980088f

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author = "Posner, {Gary H.} and Hardwin O'Dowd and Poonsakdi Ploypradith and Gumming, {Jared N.} and Suji Xie and Shapiro, {Theresa A.}",

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T1 - Antimalarial cyclic peroxy ketals

AU - Posner, Gary H.

AU - O'Dowd, Hardwin

AU - Ploypradith, Poonsakdi

AU - Gumming, Jared N.

AU - Xie, Suji

AU - Shapiro, Theresa A.

PY - 1998/6/4

Y1 - 1998/6/4

N2 - 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 anti-malarial 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.

AB - 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 anti-malarial 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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Antimalarial cyclic peroxy ketals

Abstract

ASJC Scopus subject areas

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