Succinic Acid Amides As P2-P3 Replacements For Inhibitors Of Interleukin-1 Beta Converting Enzyme (Ice Or Caspase 1)

Paul Galatsis, Bradley Caprathe,John Gilmore,Anthony Thomas,Kristin Linn,Susan Sheehan, William Harter, Catherine Kostlan,Elizabeth Lunney,Charles Stankovic,John Rubin,Kenneth Brady,Hamish Allen,Robert Talanian

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

Succinic acid amides have been found to be effective P2-P3 scaffold replacements for peptidic ICE inhibitors. Heteroarylalkyl fragments occupying the P4 position provided access to compounds with nM affinities. Utilization of an acylal prodrug moiety was required to overcome biopharmaceutical issues which led to the identification of 17f, a potential clinical candidate. (C) 2010 Elsevier Ltd. All rights reserved.

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关键词

ICE inhibitor, P2-P3 replacement, Succinic acid amides

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