title: Non-peptide alpha(v)beta(3) antagonists. Part 5: identification of potent RGD mimetics incorporating 2-aryl beta-amino acids as aspartic acid replacements.
abstract: A series of novel, highly potent alpha(v)beta(3) receptor antagonists with favorable pharmacokinetic profiles has been identified. In this series of antagonists, 2-aryl beta-amino acids function as potent aspartic acid replacements.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. karen_brashear@merck.com
authors.forename: Karen M
authors.initials: KM
authors.lastname: Brashear
authors.forename: Cecilia A
authors.initials: CA
authors.lastname: Hunt
authors.forename: Brian T
authors.initials: BT
authors.lastname: Kucer
authors.forename: Mark E
authors.initials: ME
authors.lastname: Duggan
authors.forename: George D
authors.initials: GD
authors.lastname: Hartman
authors.forename: Gideon A
authors.initials: GA
authors.lastname: Rodan
authors.forename: Sevgi B
authors.initials: SB
authors.lastname: Rodan
authors.forename: Chi-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: Andrea
authors.initials: A
authors.lastname: Barrish
authors.forename: Carl F
authors.initials: CF
authors.lastname: Homnick
authors.forename: John H
authors.initials: JH
authors.lastname: Hutchinson
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Coleman
mesh_terms: D000596:Amino Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D001224:Aspartic Acid / Q000737:chemistry; D040761:Biomimetic Materials / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D004952:Esters / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D006801:Humans; D020128:Inhibitory Concentration 50; D009842:Oligopeptides / Q000737:chemistry / Q000493:pharmacokinetics; D011485:Protein Binding; D019030:Receptors, Vitronectin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000596:Amino Acids; D004952:Esters; D009842:Oligopeptides; D019030:Receptors, Vitronectin; D001224:Aspartic Acid; C047981:arginyl-glycyl-aspartic acid