Title of article :
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
Author/Authors :
Francine Sternfeld، نويسنده , , Raymond Baker، نويسنده , , Howard B. Broughton، نويسنده , , Alexander R. Guiblin، نويسنده , , Richard A. Jelley، نويسنده , , Victor G. Matassa، نويسنده , , Austin J. Reeve، نويسنده , , Margaret S. Beer، نويسنده , , Josephine A. Stanton، نويسنده , , Richard J. Hargreaves، نويسنده , , Sara L. Shepheard، نويسنده , , Jeanette Longmore، نويسنده , , Zerin Razzaque، نويسنده , , Michael I. Graham، نويسنده , , Bindi Sohal، نويسنده , , Leslie J. Street، نويسنده ,
Abstract :
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.
