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