SYNTHESIS AND BIOLOGICAL-ACTIVITY OF 3-SUBSTITUTED 3-DESOXYNALTRINDOLE DERIVATIVES

Authors
KUBOTA H ROTHMAN RB DERSCH C MCCULLOUGH K PINTO J RICE KC
Citation
H. Kubota et al., SYNTHESIS AND BIOLOGICAL-ACTIVITY OF 3-SUBSTITUTED 3-DESOXYNALTRINDOLE DERIVATIVES, Bioorganic & medicinal chemistry letters, 8(7), 1998, pp. 799-804
Citations number
30
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
7
Year of publication
1998
Pages
799 - 804
Database
ISI
SICI code
0960-894X(1998)8:7<799:SABO33>2.0.ZU;2-E
Abstract
The 3-unsubstituted and substituted analogs of naltrindole (NTI) were synthesized using palladium-catalyzed transformations, and their bindi ng affinity to opioid receptors was determined. Although the 3-desoxy analog showed comparable delta selectivity with that of NTI, all of th e novel compounds possessed low affinity for delta receptors indicatin g the important role of the 3-oxygen atom of NTI for interaction with delta-opioid receptors. Published by Elsevier Science Ltd.