Article ID Journal Published Year Pages File Type
1377102 Bioorganic & Medicinal Chemistry Letters 2008 6 Pages PDF
Abstract

Novel ((2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamides were found to be excellent P1′ substituents in conjunction with unique constrained β-amino hydroxamic acid scaffolds for the discovery of potent selective inhibitors of TNF-α Converting Enzyme (TACE). Optimized examples proved potent for TACE, exceptionally selective over a wide panel of MMP and ADAM proteases, potent in the suppression of LPS-induced TNF-α in human whole blood and orally bioavailable.

Graphical abstractNovel ((2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamides were found to be excellent P1′ substituents in conjunction with unique constrained β-amino hydroxamic acid scaffolds for the discovery of potent, exceptionally selective inhibitors of TNF-α Converting Enzyme (TACE).Figure optionsDownload full-size imageDownload as PowerPoint slide

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