Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human β3 adrenergic receptor agonists
摘要:
Tetrahydroisoquinoline derivatives containing a 4-(hexylureido)benzenesulfonamide were examined as human beta (3) adrenergic receptor (AR) agonists. Notably, 4,4-biphenyl derivative 9 was a 6 nM full agonist of the beta (3) AR. Naphthyloxy compound 18 (beta (3) EC50 = 78 nM) did not activate the beta (1) and beta (2) ARs at 10 muM, and showed >1000-fold selectivity over binding to the beta (1) and beta (2) ARs. (C) 2000 Elsevier Science Ltd. All rights reserved.
DOI:
10.1016/s0960-894x(00)00459-5
作为产物:
描述:
二碳酸二叔丁酯 以
1,4-二氧六环 为溶剂,
以1.0 g (83%)的产率得到6-Hydroxynaphth-2-ylcarbamic acid, 1,1-dimethylethyl ester
参考文献:
名称:
Fused piperidine substituted arylsulfonamides as .beta.3-agonists
[EN] LIQUID CRYSTAL ALIGNING AGENT FOR VERTICAL ALIGNMENT, LIQUID CRYSTAL ALIGNMENT FILM, AND LIQUID CRYSTAL DISPLAY ELEMENT<br/>[FR] AGENT D'ALIGNEMENT DE CRISTAUX LIQUIDES POUR UN ALIGNEMENT VERTICAL, FILM D'ALIGNEMENT DE CRISTAUX LIQUIDES, ET ÉLÉMENT D'AFFICHAGE À CRISTAUX LIQUIDES<br/>[JA] 垂直配向用の液晶配向剤、液晶配向膜、及び液晶表示素子
Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human β3 adrenergic receptor agonists
作者:Emma R. Parmee、Linda L. Brockunier、Jiafang He、Suresh B. Singh、Mari R. Candelore、Margaret A. Cascieri、Liping Deng、Yong Liu、Laurie Tota、Matthew J. Wyvratt、Michael H. Fisher、Ann E. Weber
DOI:10.1016/s0960-894x(00)00459-5
日期:2000.10
Tetrahydroisoquinoline derivatives containing a 4-(hexylureido)benzenesulfonamide were examined as human beta (3) adrenergic receptor (AR) agonists. Notably, 4,4-biphenyl derivative 9 was a 6 nM full agonist of the beta (3) AR. Naphthyloxy compound 18 (beta (3) EC50 = 78 nM) did not activate the beta (1) and beta (2) ARs at 10 muM, and showed >1000-fold selectivity over binding to the beta (1) and beta (2) ARs. (C) 2000 Elsevier Science Ltd. All rights reserved.
Fused piperidine substituted arylsulfonamides as .beta.3-agonists
申请人:Merck & Co., Inc.
公开号:US06043253A1
公开(公告)日:2000-03-28
Fused piperidine substituted arylsulfonamides are .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for decreasing gut motility are also disclosed.