Discovery of selective indole-based prostaglandin D₂ receptor antagonist

A series of N-benzoyl-2-methylindole-3-acetic acids were synthesized and biologically evaluated as prostaglandin (PG) D₂ receptor antagonists. Some of the selected compounds significantly inhibited OVA-induced vascular permeability in guinea pig conjunctiva after oral dosing. Structure–activity rela...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2011-08, Vol.19 (15), p.4574-4588
Hauptverfasser:	Iwahashi, Maki, Shimabukuro, Atsushi, Onoda, Takahiro, Matsunaga, Yoko, Okada, Yutaka, Matsumoto, Ryoji, Nambu, Fumio, Nakai, Hisao, Toda, Masaaki
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals antagonists Biological and medical sciences Capillary Permeability - drug effects CHO Cells conjunctiva Conjunctiva - blood supply Cricetinae Cricetulus Drug Discovery Guinea Pigs Histamine and antagonists. Allergy Humans Indoles - chemistry Indoles - pharmacology Medical sciences permeability Pharmacology. Drug treatments prostaglandins Receptors, Immunologic - antagonists & inhibitors Receptors, Immunologic - metabolism Receptors, Prostaglandin - antagonists & inhibitors Receptors, Prostaglandin - metabolism structure-activity relationships
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Zusammenfassung:	A series of N-benzoyl-2-methylindole-3-acetic acids were synthesized and biologically evaluated as prostaglandin (PG) D₂ receptor antagonists. Some of the selected compounds significantly inhibited OVA-induced vascular permeability in guinea pig conjunctiva after oral dosing. Structure–activity relationship study is presented.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2011.06.014