Discovery of a new chemical lead for a matrix metalloproteinase inhibitor

…, H Habashita, T Sugiura, K Takahashi, K Ogawa…

Index: Ikura, Masahiro; Nakatani, Shingo; Yamamoto, Shingo; Habashita, Hiromu; Sugiura, Tsuneyuki; Takahashi, Kanji; Ogawa, Koji; Ohno, Hiroyuki; Nakai, Hisao; Toda, Masaaki Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 12 p. 4241 - 4252

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Citation Number: 12

Abstract

A series of N-benzoyl γ-aminobutyric hydroxamic acids were synthesized and evaluated as matrix metalloproteinase inhibitors. First, we focused on chemical modification of the N- benzoyl residue. Introduction of electron-rich para-substituents was effective to increase the inhibitory activity. Especially, some of the analogs with relatively more planar N-acyl residues, such as 10 and 11, demonstrated more potent activity. Second, chemical ...