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

Authors
BOYFIELD I COLDWELL MC HADLEY MS HEALY MAM JOHNSON CN NASH DJ RILEY GJ SCOTT EE SMITH SA STEMP G
Citation
I. Boyfield et al., NOVEL 2,5-DISUBSTITUTED-1H-PYRROLES WITH HIGH-AFFINITY FOR THE DOPAMINE D-3 RECEPTOR - N-BENZYL MODIFICATIONS, Bioorganic & medicinal chemistry letters, 7(3), 1997, pp. 327-330
Citations number
5
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
3
Year of publication
1997
Pages
327 - 330
Database
ISI
SICI code
0960-894X(1997)7:3<327:N2WHFT>2.0.ZU;2-N
Abstract
A series of 2,5-disubstituted-1H-pyrroles (4-26) has been prepared whe re the conformational requirements of the N-ethyl, N-benzyl side-chain of 1 and the effect of introducing substituents into the benzyl group have been investigated. The (R)-alpha-methylbenzyl 6 and aminoindane 10 side-chains retained high affinity for the dopamine Dg receptor, al though neither showed the selectivity of 2-phenylazacycloheptane 2. (C ) 1997, Elsevier Science Ltd.