Discovery of selective indole-based prostaglandin D 2 receptor antagonist

…, T Onoda, Y Matsunaga, Y Okada, R Matsumoto…

Index: Iwahashi, Maki; Shimabukuro, Atsushi; Onoda, Takahiro; Matsunaga, Yoko; Okada, Yutaka; Matsumoto, Ryoji; Nambu, Fumio; Nakai, Hisao; Toda, Masaaki Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 15 p. 4574 - 4588

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Citation Number: 7

Abstract

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.