Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist

Yutaka Nakajima; Hitoshi Hamashima; Ken-Ichi Washizuka; Yasuyo Tomishima; Hiroaki Ohtake; Emiko Imamura; Toshiko Miura; Hiroshi Kayakiri; Masayuki Kato

doi:10.1016/j.bmcl.2004.11.001

Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist

Bioorg Med Chem Lett. 2005 Jan 17;15(2):251-4. doi: 10.1016/j.bmcl.2004.11.001.

Authors

Yutaka Nakajima¹, Hitoshi Hamashima, Ken-Ichi Washizuka, Yasuyo Tomishima, Hiroaki Ohtake, Emiko Imamura, Toshiko Miura, Hiroshi Kayakiri, Masayuki Kato

Affiliation

¹ Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co. Ltd, 1-6, Kashima 2-Chome, Yodogawa-Ku, Osaka 532-8514, Japan. yutaka_nakajima@po.fujisawa.jp

PMID: 15603933
DOI: 10.1016/j.bmcl.2004.11.001

Abstract

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.

MeSH terms

Adrenergic beta-3 Receptor Agonists*
Adrenergic beta-Agonists / chemical synthesis*
Adrenergic beta-Agonists / pharmacology*
Animals
CHO Cells
Cricetinae
Humans
Models, Chemical
Structure-Activity Relationship

Substances

Adrenergic beta-3 Receptor Agonists
Adrenergic beta-Agonists