title: Discovery of new chemical leads for selective EP1 receptor antagonists.
abstract: A series of 4-([2-[alkyl(phenylsulfonyl)amino]phenoxy]methyl)benzoic acids were identified as functional PGE(2) antagonists with selectivity for the EP1 receptor subtype starting from a chemical lead 1, which was found while screening our in-house compound library. Discovery of the optimized analogs 21-23 is presented here and structure-activity relationships (SAR) are also discussed.
authors.affiliation: Minase Research Institute, Ono Pharmaceutical Co., Ltd, Shimamoto, Mishima, Osaka, Japan. naganawa@ono.co.jp
authors.forename: Atsushi
authors.initials: A
authors.lastname: Naganawa
authors.forename: Tetsuji
authors.initials: T
authors.lastname: Saito
authors.forename: Yuuki
authors.initials: Y
authors.lastname: Nagao
authors.forename: Hiromu
authors.initials: H
authors.lastname: Egashira
authors.forename: Maki
authors.initials: M
authors.lastname: Iwahashi
authors.forename: Tohru
authors.initials: T
authors.lastname: Kambe
authors.forename: Masatoshi
authors.initials: M
authors.lastname: Koketsu
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Yamamoto
authors.forename: Michiyoshi
authors.initials: M
authors.lastname: Kobayashi
authors.forename: Takayuki
authors.initials: T
authors.lastname: Maruyama
authors.forename: Shuichi
authors.initials: S
authors.lastname: Ohuchida
authors.forename: Hisao
authors.initials: H
authors.lastname: Nakai
authors.forename: Kigen
authors.initials: K
authors.lastname: Kondo
authors.forename: Masaaki
authors.initials: M
authors.lastname: Toda
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D001565:Benzoates / Q000138:chemical synthesis / Q000494:pharmacology*; D001665:Binding Sites; D016466:CHO Cells; D006224:Cricetinae; D018078:Receptors, Prostaglandin E / Q000037:antagonists & inhibitors* / Q000378:metabolism; D058306:Receptors, Prostaglandin E, EP1 Subtype; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000700:Analgesics; D001565:Benzoates; D018078:Receptors, Prostaglandin E; D058306:Receptors, Prostaglandin E, EP1 Subtype; D013449:Sulfonamides