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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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2011-08, Vol.19 (15), p.4574-4588
Main Authors: Iwahashi, Maki, Shimabukuro, Atsushi, Onoda, Takahiro, Matsunaga, Yoko, Okada, Yutaka, Matsumoto, Ryoji, Nambu, Fumio, Nakai, Hisao, Toda, Masaaki
Format: Article
Language:English
Subjects:
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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Summary: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