Synthesis of hexahydrocyclopentimidazol-2-(1 H)-one derivatives displaying selective DP-receptor agonist properties

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 a...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 1996, Vol.4 (1), p.81-90
Hauptverfasser:	Barraclough, Paul, Bolofo, Mary L., Giles, Heather, Gillam, Janet, John Harris, C., Kelly, Michael G., Leff, Paul, McNeill, Alan, Robertson, Alan D., Stepney, Ray J., Whittle, Brendan J.R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Blood Pressure - drug effects Butyrates - chemical synthesis Butyrates - chemistry Butyrates - pharmacology Drug Design Humans Hydantoins - chemistry Hydantoins - pharmacology Imidazoles - chemical synthesis Imidazoles - chemistry Imidazoles - pharmacology Jugular Veins - drug effects Jugular Veins - metabolism Platelet Aggregation - drug effects Platelet Aggregation Inhibitors - chemical synthesis Platelet Aggregation Inhibitors - chemistry Platelet Aggregation Inhibitors - pharmacology Rabbits Rats Receptors, Prostaglandin - agonists Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/0968-0896(95)00173-5