Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist.
The discovery of a novel, potent and selective beta(3)-adrenergic receptor (AR) agonist is described. SAR studies demonstrated the structural requirements for activity and selectivity. Compound 1c, which showed good beta(3)-AR activity and selectivity, was identified and pharmacokinetics were investigated.
Nakajima
Yutaka
Y
Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co. Ltd, 1-6, Kashima 2-Chome, Yodogawa-Ku, Osaka 532-8514, Japan. yutaka_nakajima@po.fujisawa.jp
Hamashima
Hitoshi
H
Washizuka
Ken-Ichi
K
Tomishima
Yasuyo
Y
Ohtake
Hiroaki
H
Imamura
Emiko
E
Miura
Toshiko
T
Kayakiri
Hiroshi
H
Kato
Masayuki
M
D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D006801:Humans; D008956:Models, Chemical; D013329:Structure-Activity Relationship
D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists