Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity

A series of 8-substituted benzodifuran analogs was prepared and evaluated for 5-HT(2A) receptor binding and activation. Several compounds containing ether and ester functionality were found to be potent agonists. Topical ocular administration of 5, 18, and 25 effectively reduced intra-ocular pressur...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-06, Vol.17 (11), p.2998-3002
Hauptverfasser:	ZIXIA FENG, MOHAPATRA, Suchismita, KLIMKO, Peter G, HELLBERG, Mark R, MAY, Jesse A, KELLY, Curtis, WILLIAMS, Gary, MCLAUGHLIN, Marsha A, SHARIF, Najam A
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antihypertensive Agents - chemical synthesis Antihypertensive Agents - chemistry Antihypertensive Agents - pharmacology Benzofurans - chemical synthesis Benzofurans - chemistry Benzofurans - pharmacology Biological and medical sciences Eye Macaca fascicularis Medical sciences Muscle, Smooth, Vascular - cytology Muscle, Smooth, Vascular - drug effects Ocular Hypertension Pharmacology. Drug treatments Rats Receptor, Serotonin, 5-HT2A - chemistry Serotonin 5-HT2 Receptor Agonists Serotonin Receptor Agonists - chemical synthesis Serotonin Receptor Agonists - chemistry Serotonin Receptor Agonists - pharmacology Structure-Activity Relationship
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Zusammenfassung:	A series of 8-substituted benzodifuran analogs was prepared and evaluated for 5-HT(2A) receptor binding and activation. Several compounds containing ether and ester functionality were found to be potent agonists. Topical ocular administration of 5, 18, and 25 effectively reduced intra-ocular pressure in the hypertensive cynomolgus monkey eye in the range of 25-37%.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.03.073