title: Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements.
abstract: Potent non-peptidic alpha(v)beta(3) antagonists have been prepared incorporating various beta-amino acids as aspartic acid mimetics. Modification of the beta-alanine 3-substituents alters the potency and physicochemical properties of these receptor antagonists and in some cases provides orally bioavailable alpha(v)beta(3) 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: Karen M
authors.initials: KM
authors.lastname: Brashear
authors.forename: Cecilia A
authors.initials: CA
authors.lastname: Hunt
authors.forename: William F
authors.initials: WF
authors.lastname: Hoffman
authors.forename: John H
authors.initials: JH
authors.lastname: Hutchinson
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Breslin
authors.forename: Carol A
authors.initials: CA
authors.lastname: McVean
authors.forename: Ben C
authors.initials: BC
authors.lastname: Askew
authors.forename: George D
authors.initials: GD
authors.lastname: Hartman
authors.forename: Sevgi B
authors.initials: SB
authors.lastname: Rodan
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: Bennett
authors.initials: B
authors.lastname: Ma
authors.forename: Laura A
authors.initials: LA
authors.lastname: Libby
authors.forename: Kara M
authors.initials: KM
authors.lastname: Merkle
authors.forename: Gary L
authors.initials: GL
authors.lastname: Stump
authors.forename: Audrey A
authors.initials: AA
authors.lastname: Wallace
authors.forename: Joseph J
authors.initials: JJ
authors.lastname: Lynch
authors.forename: Robert
authors.initials: R
authors.lastname: Lynch
authors.forename: Mark E
authors.initials: ME
authors.lastname: Duggan
mesh_terms: D000596:Amino Acids / Q000737:chemistry; D000818:Animals; D001224:Aspartic Acid; D001667:Binding, Competitive; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D006801:Humans; D020128:Inhibitory Concentration 50; D018716:Molecular Mimicry; D009842:Oligopeptides / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D010024:Osteoporosis / Q000517:prevention & control; D011485:Protein Binding; D019030:Receptors, Vitronectin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000596:Amino Acids; D009842:Oligopeptides; D019030:Receptors, Vitronectin; D001224:Aspartic Acid; C047981:arginyl-glycyl-aspartic acid