Tetrahydroisoquinoline-3-carboxylate based matrix-metalloproteinase inhibitors: design, synthesis and structure–activity relationship

…, M Schudok, W Schwab, W Thorwart, D Barbier…

Index: Matter, Hans; Schudok, Manfred; Schwab, Wilfried; Thorwart, Werner; Barbier, Denis; Billen, Guenter; Haase, Burkhard; Neises, Bernhard; Weithmann, Klaus-Ulrich; Wollmann, Theo Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 11 p. 3529 - 3544

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Citation Number: 49

Abstract

The design, synthesis and structure–activity relationship (SAR) of a series of nonpeptidic 2- arylsulfonyl-1, 2, 3, 4-tetrahydro-isoquinoline-3-carboxylates and-hydroxamates as inhibitors of the matrix metalloproteinase human neutrophil collagenase (MMP-8) is described here. Based on available X-ray structures of MMP-8/inhibitor complexes, our structure-based design strategy was directed to complement major protein-ligand interaction regions ...