Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373303 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
As an extension of research, we have investigated modification of left-hand side (LHS) of biphenyl analogues containing an acylsulfonamide moiety in the development of potent and selective human β3-adrenergic receptor (AR) agonists. Result of structure–activity relationships (SAR) and cassette-dosing evaluation in dogs showed that the hydroxynorephedrine analogue 16 had an excellent balance of in vitro and in vivo potency with pharmacokinetic profiles. In addition, to facilitate structure-based drug design (SBDD), we also have performed a docking study of biphenyl analogues based on the X-ray structure of the β2-adrenergic receptor.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kouji Hattori, Masaya Orita, Susumu Toda, Masashi Imanishi, Shinji Itou, Yutaka Nakajima, Daisuke Tanabe, Kenichi Washizuka, Takanobu Araki, Minoru Sakurai, Shigeo Matsui, Emiko Imamura, Koji Ueshima, Takao Yamamoto, Nobuhiro Yamamoto, Hirofumi Ishikawa,