ChemInform Abstract: 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

Autor:	Z. Razzaque, Richard Hargreaves, Leslie J. Street, Richard Alexander Jelley, Josephine A. Stanton, Bindi Sohal, S. L. Shepheard, Victor G. Matassa, Jeanette Longmore, Alexander Richard Guiblin, Francine Sternfeld, Raymond Baker, Austin John Reeve, Margaret S. Beer, Michael I. Graham, Howard B. Broughton
Rok vydání:	2010
Předmět:	Indole test Agonist Chemistry medicine.drug_class Stereochemistry Substituent Triazole General Medicine Tryptamines chemistry.chemical_compound medicine Ethylamine Selectivity Receptor
Zdroj:	ChemInform. 27
ISSN:	0931-7597
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::74847d6bfb22278ab8881dec6ddab101 https://doi.org/10.1002/chin.199649147 Zobrazit plný text záznamu Plný text