title: Synthesis of Hexahydrocyclopentimidazol-2-(1H)-one derivatives displaying selective DP-receptor agonist properties.
abstract: The rationale for investigating conformationally restricted analogues of BW245C as DP-receptor ligands and the syntheses of three such racemic bicyclic imidazolidinone analogues are described. Compounds 7 (BW587C), 8 (BW480C85), and 9 (BW572C85) were found to be potent inhibitors of human platelet aggregation and selective DP-receptor agonists in washed platelet and jugular vein isolated tissue assays.
authors.affiliation: Department of Medicinal Chemistry, Wellcome Research Laboratories, Beckenham, Kent, U.K.
authors.forename: P
authors.initials: P
authors.lastname: Barraclough
authors.forename: M L
authors.initials: ML
authors.lastname: Bolofo
authors.forename: H
authors.initials: H
authors.lastname: Giles
authors.forename: J
authors.initials: J
authors.lastname: Gillam
authors.forename: C J
authors.initials: CJ
authors.lastname: Harris
authors.forename: M G
authors.initials: MG
authors.lastname: Kelly
authors.forename: P
authors.initials: P
authors.lastname: Leff
authors.forename: A
authors.initials: A
authors.lastname: McNeill
authors.forename: A D
authors.initials: AD
authors.lastname: Robertson
authors.forename: R J
authors.initials: RJ
authors.lastname: Stepney
authors.forename: B J
authors.initials: BJ
authors.lastname: Whittle
mesh_terms: D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D002087:Butyrates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D006801:Humans; D006827:Hydantoins / Q000737:chemistry / Q000494:pharmacology; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007601:Jugular Veins / Q000187:drug effects / Q000378:metabolism; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D011982:Receptors, Prostaglandin / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: C100557:BW 480C85; C100558:BW 572C85; C100556:BW 587C; D002087:Butyrates; D006827:Hydantoins; D007093:Imidazoles; D010975:Platelet Aggregation Inhibitors; D011982:Receptors, Prostaglandin; C030669:BW 245C