title: Design and synthesis of conformationally-constrained MMP inhibitors.
abstract: A novel series of conformationally constrained matrix metalloprotease inhibitors was identified. The potencies observed for these inhibitors were highly dependent upon the substitution pattern on the caprolactam ring as well as the succinate moiety.
authors.affiliation: Procter and Gamble Pharmaceuticals, Health Care Research Center, Mason, OH 45040, USA.
authors.forename: M G
authors.initials: MG
authors.lastname: Natchus
authors.forename: M
authors.initials: M
authors.lastname: Cheng
authors.forename: C T
authors.initials: CT
authors.lastname: Wahl
authors.forename: S
authors.initials: S
authors.lastname: Pikul
authors.forename: N G
authors.initials: NG
authors.lastname: Almstead
authors.forename: R S
authors.initials: RS
authors.lastname: Bradley
authors.forename: Y O
authors.initials: YO
authors.lastname: Taiwo
authors.forename: G E
authors.initials: GE
authors.lastname: Mieling
authors.forename: C M
authors.initials: CM
authors.lastname: Dunaway
authors.forename: C E
authors.initials: CE
authors.lastname: Snider
authors.forename: J M
authors.initials: JM
authors.lastname: McIver
authors.forename: B L
authors.initials: BL
authors.lastname: Barnett
authors.forename: S J
authors.initials: SJ
authors.lastname: McPhail
authors.forename: M B
authors.initials: MB
authors.lastname: Anastasio
authors.forename: B
authors.initials: B
authors.lastname: De
mesh_terms: D002209:Caprolactam / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017364:Collagenases / Q000737:chemistry; D015195:Drug Design; D007202:Indicators and Reagents; D007700:Kinetics; D020781:Matrix Metalloproteinase 1; D019278:Matrix Metalloproteinase 3 / Q000737:chemistry; D061965:Matrix Metalloproteinase Inhibitors; D008666:Metalloendopeptidases / Q000037:antagonists & inhibitors*; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D011487:Protein Conformation; D013329:Structure-Activity Relationship; D013386:Succinates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D007202:Indicators and Reagents; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors; D013386:Succinates; D002209:Caprolactam; D017364:Collagenases; D008666:Metalloendopeptidases; D019278:Matrix Metalloproteinase 3; D020781:Matrix Metalloproteinase 1