title: Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics.
abstract: Potent non-peptidic alpha(v)beta(3) antagonists have been prepared where deletion of an amide bond from an earlier series of linear RGD-mimetics provides a novel series of chain-shortened alpha(v)beta(3) antagonists with significantly improved oral pharmacokinetics. These chain-shortened alpha(v)beta(3) antagonists represent structurally novel integrin inhibitors.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. paul_coleman@merck.com
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Coleman
authors.forename: Ben C
authors.initials: BC
authors.lastname: Askew
authors.forename: John H
authors.initials: JH
authors.lastname: Hutchinson
authors.forename: David B
authors.initials: DB
authors.lastname: Whitman
authors.forename: James J
authors.initials: JJ
authors.lastname: Perkins
authors.forename: George D
authors.initials: GD
authors.lastname: Hartman
authors.forename: Gideon A
authors.initials: GA
authors.lastname: Rodan
authors.forename: Chih-Tai
authors.initials: CT
authors.lastname: Leu
authors.forename: Thomayant
authors.initials: T
authors.lastname: Prueksaritanont
authors.forename: Carmen
authors.initials: C
authors.lastname: Fernandez-Metzler
authors.forename: Kara M
authors.initials: KM
authors.lastname: Merkle
authors.forename: Robert
authors.initials: R
authors.lastname: Lynch
authors.forename: Joseph J
authors.initials: JJ
authors.lastname: Lynch
authors.forename: Sevgi B
authors.initials: SB
authors.lastname: Rodan
authors.forename: Mark E
authors.initials: ME
authors.lastname: Duggan
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004285:Dogs; D006207:Half-Life; D020128:Inhibitory Concentration 50; D039302:Integrin alphaVbeta3 / Q000037:antagonists & inhibitors*; D008657:Metabolic Clearance Rate; D018716:Molecular Mimicry; D009842:Oligopeptides / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D039302:Integrin alphaVbeta3; D009842:Oligopeptides; C047981:arginyl-glycyl-aspartic acid