Bioorganic & Medicinal Chemistry Letters 2000-10-16

Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists.

E R Parmee, L L Brockunier, J He, S B Singh, M R Candelore, M A Cascieri, L Deng, Y Liu, L Tota, M J Wyvratt, M H Fisher, A E Weber

文献索引：Bioorg. Med. Chem. Lett. 10(20) , 2283-6, (2000)

全文：HTML全文

摘要

Tetrahydroisoquinoline derivatives containing a 4-(hexylureido)benzenesulfonamide were examined as human beta3 adrenergic receptor (AR) agonists. Notably, 4,4-biphenyl derivative 9 was a 6 nM full agonist of the beta3 AR. Naphthyloxy compound 18 (beta3 EC50 = 78 nM) did not activate the beta1 and beta2 ARs at 10 microM, and showed >1000-fold selectivity over binding to the beta1 and beta2 ARs.