title: Discovery of novel series of benzoic acid derivatives containing biphenyl ether moiety as potent and selective human beta(3)-adrenergic receptor agonists: Part IV.
abstract: Identification and SAR study of novel series of beta(3)-AR agonists with benzoic acid are described. Conversion of ether linkage position of phenoxybenzoic acid derivative 2b led to compound 7b with moderate beta(3)-AR activity. Further modification in right, center and left parts of compound 7b was investigated to improve the beta(3)-AR potency and selectivity. Compounds 7g and 7k, with the bulky aliphatic-substituted group at 2-position of benzoic acid moiety, were identified as potent and selective beta(3)-AR agonists. In addition, in vivo efficacy of compounds 7g and 7k was exhibited on dog OAB model.
authors.affiliation: Chemistry Research Laboratories, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.
authors.forename: Yutaka
authors.initials: Y
authors.lastname: Nakajima
authors.forename: Masashi
authors.initials: M
authors.lastname: Imanishi
authors.forename: Shinji
authors.initials: S
authors.lastname: Itou
authors.forename: Hitoshi
authors.initials: H
authors.lastname: Hamashima
authors.forename: Yasuyo
authors.initials: Y
authors.lastname: Tomishima
authors.forename: Kenichi
authors.initials: K
authors.lastname: Washizuka
authors.forename: Minoru
authors.initials: M
authors.lastname: Sakurai
authors.forename: Shigeo
authors.initials: S
authors.lastname: Matsui
authors.forename: Emiko
authors.initials: E
authors.lastname: Imamura
authors.forename: Koji
authors.initials: K
authors.lastname: Ueshima
authors.forename: Takao
authors.initials: T
authors.lastname: Yamamoto
authors.forename: Nobuhiro
authors.initials: N
authors.lastname: Yamamoto
authors.forename: Hirofumi
authors.initials: H
authors.lastname: Ishikawa
authors.forename: Keiko
authors.initials: K
authors.lastname: Nakano
authors.forename: Naoko
authors.initials: N
authors.lastname: Unami
authors.forename: Kaori
authors.initials: K
authors.lastname: Hamada
authors.forename: Kouji
authors.initials: K
authors.lastname: Hattori