Development of a prostaglandin D 2 receptor antagonist: discovery of a new chemical lead

K Torisu, K Kobayashi, M Iwahashi, H Egashira…

Index: Torisu, Kazuhiko; Kobayashi, Kaoru; Iwahashi, Maki; Egashira, Hiromu; Nakai, Yoshihiko; Okada, Yutaka; Nanbu, Fumio; Ohuchida, Shuichi; Nakai, Hisao; Toda, Masaaki European Journal of Medicinal Chemistry, 2005 , vol. 40, # 5 p. 505 - 519

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Citation Number: 20

Abstract

A series of N-(p-alkoxy) benzoyl-5-methoxy-2-methylindole-3-acetic acids and N-(p-butoxy) benzoyl-2-methylindole-4-acetic acid were discovered as new chemical leads for a prostaglandin D2 (PGD2) receptor antagonist. Most of them exhibited PGD2 receptor binding and blocked cyclic adenosine 3′, 5′-monophosphate (cAMP) formation in vitro. In particular, 2-methylindole-4-acetic acid analog 1 showed markedly increased receptor ...