Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2010 Feb 1;20(3):832-5. doi: 10.1016/j.bmcl.2009.12.094. Epub 2010 Jan 4.

Remote functionalization of SCH 39166: discovery of potent and selective benzazepine dopamine D1 receptor antagonists.

Author information

1
Department of Medicinal Chemistry and Metabolic Disorders, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. sasikumartk@yahoo.com

Abstract

A series of novel benzazepine derived dopamine D(1) antagonists have been discovered. These compounds are highly potent at D(1) and showed excellent selectivity over D(2) and D(4) receptors. SAR studies revealed that a variety of functional groups are tolerated on the D-ring of known tetracyclic benzazepine analog 2, SCH 39166, leading to compounds with nanomolar potency at D(1) and good selectivity over D(2)-like receptors.

PMID:
20064718
DOI:
10.1016/j.bmcl.2009.12.094
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center