title: Design and Synthesis of Non-peptide RGD Mimics for Evaluation of Their Utility as Anti-platelet Agents.
abstract: Arg-Gly-Asp (RGD) mimics were synthesized and their anti-platelet activity was evaluated. A concise method was developed for the synthesis of the target compounds from dehydroepiandrosterone and Wieland-Miescher and Hajos-Parrish ketones, which are suitable for readily available platform. Among the synthesized compounds, the perhydronaphthalene framework with a 3-(4-piperidinyl)propoxyl structure 3e possessed the highest anti-aggregative activity. The IC50values of 3e were 0.91 mM (ADP initiation) and 0.54 mM (collagen initiation).
authors.affiliation: Meiji Pharmaceutical University.
authors.forename: Kazuhiro
authors.initials: K
authors.lastname: Higuchi
authors.forename: Hideki
authors.initials: H
authors.lastname: Hikita
authors.forename: Asumi
authors.initials: A
authors.lastname: Murayama
authors.forename: Daichi
authors.initials: D
authors.lastname: Yuri
authors.forename: Natsu
authors.initials: N
authors.lastname: Kobayakawa
authors.forename: Takashi
authors.initials: T
authors.lastname: Takahashi
authors.forename: Shigeru
authors.initials: S
authors.lastname: Kojima
authors.forename: Hiroko
authors.initials: H
authors.lastname: Ueno
authors.forename: Tomomi
authors.initials: T
authors.lastname: Hatakeyama
authors.forename: Airi
authors.initials: A
authors.lastname: Kato
authors.forename: Masanori
authors.initials: M
authors.lastname: Tayu
authors.forename: Etsuko
authors.initials: E
authors.lastname: Oyama
authors.forename: Shigeo
authors.initials: S
authors.lastname: Sugiyama
authors.forename: Kazuyuki
authors.initials: K
authors.lastname: Ishii
authors.forename: Hidenobu
authors.initials: H
authors.lastname: Takahashi
authors.forename: Tomomi
authors.initials: T
authors.lastname: Kawasaki
mesh_terms: D001792:Blood Platelets / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D008968:Molecular Conformation; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D009842:Oligopeptides; D010975:Platelet Aggregation Inhibitors; C047981:arginyl-glycyl-aspartic acid