TETRACYCLIC ANALOGS OF [-S14297 - SYNTHESIS AND DETERMINATION OF AFFINITY AND SELECTIVITY AT CLONED HUMAN DOPAMINE D-3 VS D-2 RECEPTORS(])

Authors
PEGLION JL VIAN J GOUMENT B DESPAUX N AUDINOT V MILLAN MJ
Citation
Jl. Peglion et al., TETRACYCLIC ANALOGS OF [-S14297 - SYNTHESIS AND DETERMINATION OF AFFINITY AND SELECTIVITY AT CLONED HUMAN DOPAMINE D-3 VS D-2 RECEPTORS(]), Bioorganic & medicinal chemistry letters, 7(7), 1997, pp. 881-886
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
7
Year of publication
1997
Pages
881 - 886
Database
ISI
SICI code
0960-894X(1997)7:7<881:TAO[-S>2.0.ZU;2-D
Abstract
Starting from the structure of the preferential D-3 antagonist S 14297 (1), we have prepared a series of cis and trans tetracyclic derivativ es of general formula I in order to improve potency and selectivity fo r D-3 receptors. The trans oxazino derivative 2c, showed slightly incr eased affinity at D-3 receptors and double the selectivity for D-3 ove r D-2 receptors, in comparison to S 14297. Cis derivatives and compoun ds where R-1 is aralkyl were totally devoid of activity. (C) 1997 Else vier Science Ltd.