Discovery of selective indole-based prostaglandin D sub(2 receptor antagonist)

Discovery of selective indole-based prostaglandin D sub(2 receptor antagonist)

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

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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
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Sprache:eng
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Zusammenfassung:A series of N-benzoyl-2-methylindole-3-acetic acids were synthesized and biologically evaluated as prostaglandin (PG) D sub(2 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
DOI:10.1016/j.bmc.2011.06.014