The chemical evolution of N,N-dimethyl-2-[5-(1,2,4-triazol-4-yl)-1H-indol-3-yl]ethylamine (L-741,604) and analogues: Potent and selective agonists for 5-HT1D receptors

被引：21

作者：

Sternfeld, F ^{[1
]}

Baker, R ^{[1
]}

Broughton, HB ^{[1
]}

Guiblin, AR ^{[1
]}

Jelley, RA ^{[1
]}

Matassa, VG ^{[1
]}

Reeve, AJ ^{[1
]}

Beer, MS ^{[1
]}

Stanton, JA ^{[1
]}

Hargreaves, RJ ^{[1
]}

Shepheard, SL ^{[1
]}

Longmore, J ^{[1
]}

Razzaque, Z ^{[1
]}

Graham, MI ^{[1
]}

Sohal, B ^{[1
]}

Street, LJ ^{[1
]}

机构：

[1] MERCK SHARP & DOHME LTD,RES LABS,BIOCHEM & PHARMACOL DEPT,NEUROSCI RES CTR,HARLOW CM20 2QR,ESSEX,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 15期

关键词：

D O I：

10.1016/0960-894X(96)00324-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Optimisation of a series of 5-(heterocyclyl)tryptamines led to the identification of the symmetrically substituted, N-4 linked 1,2,4-triazole as the best indole C-5 substituent for 5-HT1D receptor affinity and selectivity. The triazole (8) is the most potent and selective, orally bioavailable, 5-HT1D receptor agonist identified to date, showing an order of magnitude greater potency than the clinical compound sumatriptan with improved subtype selectivity. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：1825 / 1830

页数：6

共 19 条

[1]

BAKER R, 1994, Patent No. 581538

[2] TRANSAMINATIONS OF NN-DIMETHYLFORMAMIDE AZINE [J].