Potent, exceptionally selective, orally bioavailable inhibitors of TNF-α converting enzyme (TACE): novel 2-substituted-1H-benzo [d] imidazol-1-yl) methyl) benzamide …

…, Z Lu, R Anand, RQ Liu, MB Covington, K Vaddi…

Index: Ott, Gregory R.; Asakawa, Naoyuki; Lu, Zhonghui; Anand, Rajan; Liu, Rui-Qin; Covington, Maryanne B.; Vaddi, Krishna; Qian, Mingxin; Newton, Robert C.; Christ, David D.; Trzaskos, James M.; Duan, James J.-W. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 5 p. 1577 - 1582

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Citation Number: 27

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 ...