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Bioorg Med Chem Lett. 2010 Feb 1;20(3):836-40. doi: 10.1016/j.bmcl.2009.12.100. Epub 2010 Jan 4.

Discovery of new SCH 39166 analogs as potent and selective dopamine D1 receptor antagonists.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.

Abstract

A series of novel dopamine D(1) antagonists derived from functionalization of the D-ring of SCH 39166 were prepared. A number of these compounds displayed subnanomolar D(1) activity and more than 1000-fold selectivity over D(2). We found C-3 derivatization afforded compounds with superior overall profile in comparison to the C-2 and C-4 derivatization. A number of highly potent D(1) antagonists were discovered which have excellent selectivity over other dopamine receptors and improved PK profile compared to SCH 39166.

PMID:
20061148
DOI:
10.1016/j.bmcl.2009.12.100
[Indexed for MEDLINE]

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