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Bioorg Med Chem Lett. 2010 Apr 15;20(8):2474-7. doi: 10.1016/j.bmcl.2010.03.004. Epub 2010 Mar 10.

A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties.

Author information

1
Merck Research Laboratories, Kenilworth, NJ 07033, USA. sasikumartk@yahoo.com

Abstract

A-ring modifications on the triazafluorenone core structure were investigated. Five membered heterocycles such as pyrazoles and isothiazoles are not tolerated. It has been found that the pyrimidine nucleus was very well tolerated on the left hand side. Amino pyrimidine compounds 24 and 27 showed acceptable PK profile with significant brain penetration. Compound 9 served as a versatile intermediate for a number of chemical transformations.

PMID:
20346665
DOI:
10.1016/j.bmcl.2010.03.004
[Indexed for MEDLINE]

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