NOVEL 2,5-DISUBSTITUTED-1H-PYRROLES WITH HIGH-AFFINITY FOR THE DOPAMINE D-3 RECEPTOR

Authors
BOLTON D BOYFIELD I COLDWELL MC HADLEY MS HEALY MAM JOHNSON CN MARKWELL RE NASH DJ RILEY GJ STEMP G WADSWORTH HJ
Citation
D. Bolton et al., NOVEL 2,5-DISUBSTITUTED-1H-PYRROLES WITH HIGH-AFFINITY FOR THE DOPAMINE D-3 RECEPTOR, Bioorganic & medicinal chemistry letters, 6(11), 1996, pp. 1233-1236
Citations number
6
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
11
Year of publication
1996
Pages
1233 - 1236
Database
ISI
SICI code
0960-894X(1996)6:11<1233:N2WHFT>2.0.ZU;2-L
Abstract
A series of 2,5-disubstituted-1H-pyrroles (4-18) has been prepared bas ed on replacement of the amide of sultopride 1 by a pyrrole ring. Subs equent modification of the basic side chain gave compounds with high a ffinity for the dopamine D-3 receptor. In addition, 12 and 17 were sho wn to be D-3 antagonists with 30-fold selectivity for the D-3 receptor over the D-2 receptor. Copyright (C) 1996 Elsevier Science Ltd