title: Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.
abstract: A series of succinyl hydroxamate MMP inhibitors were prepared incorporating an aryl amino ketone moiety in place of the more typical C-terminal amino acid amides. Compounds of the C-terminal ketone series displayed potent inhibition of MMPs. Several compounds of the series were shown to be orally bioavailable.
authors.affiliation: Department 47J, AP-10, Abbott Laboratory, Abbott Park, Illinois 60064, USA.
authors.forename: G S
authors.initials: GS
authors.lastname: Sheppard
authors.forename: A S
authors.initials: AS
authors.lastname: Florjancic
authors.forename: J R
authors.initials: JR
authors.lastname: Giesler
authors.forename: L
authors.initials: L
authors.lastname: Xu
authors.forename: Y
authors.initials: Y
authors.lastname: Guo
authors.forename: S K
authors.initials: SK
authors.lastname: Davidsen
authors.forename: P A
authors.initials: PA
authors.lastname: Marcotte
authors.forename: I
authors.initials: I
authors.lastname: Elmore
authors.forename: D H
authors.initials: DH
authors.lastname: Albert
authors.forename: T J
authors.initials: TJ
authors.lastname: Magoc
authors.forename: J J
authors.initials: JJ
authors.lastname: Bouska
authors.forename: C L
authors.initials: CL
authors.lastname: Goodfellow
authors.forename: D W
authors.initials: DW
authors.lastname: Morgan
authors.forename: J B
authors.initials: JB
authors.lastname: Summers
mesh_terms: D018093:Gelatinases / Q000037:antagonists & inhibitors*; D006877:Hydroxamic Acids / Q000494:pharmacology*; D007659:Ketones / Q000494:pharmacology*; D020781:Matrix Metalloproteinase 1; D020778:Matrix Metalloproteinase 2; D020783:Matrix Metalloproteinase 7; D061965:Matrix Metalloproteinase Inhibitors; D008666:Metalloendopeptidases / Q000037:antagonists & inhibitors*; D011480:Protease Inhibitors / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D006877:Hydroxamic Acids; D007659:Ketones; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors; D018093:Gelatinases; D008666:Metalloendopeptidases; D020783:Matrix Metalloproteinase 7; D020778:Matrix Metalloproteinase 2; D020781:Matrix Metalloproteinase 1