Bioorganic and Medicinal Chemistry Letters p. 1825 - 1830 (1996)
Update date:2022-08-04
Topics:
Sternfeld, Francine
Baker, Raymond
Broughton, Howard B.
Guiblin, Alexander R.
Jelley, Richard A.
Matassa, Victor G.
Reeve, Austin J.
Beer, Margaret S.
Stanton, Josephine A.
Hargreaves, Richard J.
Shepheard, Sara L.
Longmore, Jeanette
Razzaque, Zerin
Graham, Michael I.
Sohal, Bindi
Street, Leslie J.
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-HT(1D) receptor affinity and selectivity. The triazole (8) is the most potent and selective, orally bioavailable, 5-HT(1D) receptor agonist identified to date, showing an order of magnitude greater potency than the clinical compound sumatriptan with improved subtype selectivity.
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(2014)