461665-34-9Relevant academic research and scientific papers
Potent, exceptionally selective, orally bioavailable inhibitors of TNF-α Converting Enzyme (TACE): Novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1′ substituents
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.
, p. 1577 - 1582 (2008)
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.
