title: Discovery of orally active prostaglandin D2 receptor antagonists.
abstract: A series of N-(p-alkoxy)benzoyl-2-methylindole-4-acetic acids were synthesized and evaluated for prostaglandin D(2) (DP) receptor affinity and antagonist activity. Some of them exhibited strong receptor binding and were potent in the cAMP formation assays. These antagonists also suppressed allergic inflammatory responses such as the PGD(2)-induced increase of microvascular permeability. Structure-activity relationship (SAR) data are presented.
authors.affiliation: Minase Research Institute, Ono Pharmaceutical Co., Ltd, Shimamoto, Osaka, Mishima 618-8585, Japan. torisu@ono.co.jp
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Torisu
authors.forename: Kaoru
authors.initials: K
authors.lastname: Kobayashi
authors.forename: Maki
authors.initials: M
authors.lastname: Iwahashi
authors.forename: Yoshihiko
authors.initials: Y
authors.lastname: Nakai
authors.forename: Takahiro
authors.initials: T
authors.lastname: Onoda
authors.forename: Toshihiko
authors.initials: T
authors.lastname: Nagase
authors.forename: Isamu
authors.initials: I
authors.lastname: Sugimoto
authors.forename: Yutaka
authors.initials: Y
authors.lastname: Okada
authors.forename: Ryoji
authors.initials: R
authors.lastname: Matsumoto
authors.forename: Fumio
authors.initials: F
authors.lastname: Nanbu
authors.forename: Shuichi
authors.initials: S
authors.lastname: Ohuchida
authors.forename: Hisao
authors.initials: H
authors.lastname: Nakai
authors.forename: Masaaki
authors.initials: M
authors.lastname: Toda
mesh_terms: D000284:Administration, Oral; D000818:Animals; D018926:Anti-Allergic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002199:Capillary Permeability; D006168:Guinea Pigs; D006801:Humans; D051379:Mice; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D018926:Anti-Allergic Agents; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; C036293:prostaglandin D2 receptor