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Bioorg Med Chem Lett. 2009 Jun 15;19(12):3199-203. doi: 10.1016/j.bmcl.2009.04.104. Epub 2009 May 3.

Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain.

Author information

1
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. sasikumartk@yahoo.com

Abstract

Introduction of small unsaturated alkylamino groups at the 4-position of the A-ring of the tricyclic framework (triazafluorenone) afforded extremely potent and selective mGluR1 antagonists with desirable properties. Compounds 11q and 11s are active in the SNL pain model with ED(50)s 3.3 and 6.4 mg/kg respectively. Metabolic outcome of propargyl amino moiety was studied.

PMID:
19433355
DOI:
10.1016/j.bmcl.2009.04.104
[Indexed for MEDLINE]

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