title: The discovery of anthranilic acid-based MMP inhibitors. Part 1: SAR of the 3-position.
abstract: A novel series of anthranilic acid-based inhibitors of MMP-1, MMP-9, and MMP-13 was prepared and evaluated both in vitro and in vivo. The most potent compound, 6e, has in vivo activity in a rat sponge-wrapped cartilage model.
authors.affiliation: Wyeth-Ayerst Research, Pearl River, NY 10965, USA. levinji@war.wyeth.com
authors.forename: J I
authors.initials: JI
authors.lastname: Levin
authors.forename: M T
authors.initials: MT
authors.lastname: Du
authors.forename: J F
authors.initials: JF
authors.lastname: DiJoseph
authors.forename: L M
authors.initials: LM
authors.lastname: Killar
authors.forename: A
authors.initials: A
authors.lastname: Sung
authors.forename: T
authors.initials: T
authors.lastname: Walter
authors.forename: M A
authors.initials: MA
authors.lastname: Sharr
authors.forename: C E
authors.initials: CE
authors.lastname: Roth
authors.forename: F J
authors.initials: FJ
authors.lastname: Moy
authors.forename: R
authors.initials: R
authors.lastname: Powers
authors.forename: G
authors.initials: G
authors.lastname: Jin
authors.forename: R
authors.initials: R
authors.lastname: Cowling
authors.forename: J S
authors.initials: JS
authors.lastname: Skotnicki
mesh_terms: D000818:Animals; D020650:Combinatorial Chemistry Techniques; D006801:Humans; D006877:Hydroxamic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D053509:Matrix Metalloproteinase 13; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D062367:ortho-Aminobenzoates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D006877:Hydroxamic Acids; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors; D013449:Sulfonamides; D062367:ortho-Aminobenzoates; C031385:anthranilic acid; C507079:MMP13 protein, human; D053509:Matrix Metalloproteinase 13; C507083:Mmp13 protein, rat