Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation

Steven L Roach; Robert I Higuchi; Andrew R Hudson; Angie Vassar; Virginia H S Grant; Ryan Lamer; Charlene Hooper; Deepa Rungta; Peter M Syka; Dale E Mais; Keith B Marschke; Lin Zhi

doi:10.1016/j.bmcl.2011.01.106

Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1658-62. doi: 10.1016/j.bmcl.2011.01.106. Epub 2011 Jan 27.

Authors

Steven L Roach¹, Robert I Higuchi, Andrew R Hudson, Angie Vassar, Virginia H S Grant, Ryan Lamer, Charlene Hooper, Deepa Rungta, Peter M Syka, Dale E Mais, Keith B Marschke, Lin Zhi

Affiliation

¹ Discovery Research, Ligand Pharmaceuticals, La Jolla, CA 92037, USA. sroach@ligand.com

PMID: 21349714
DOI: 10.1016/j.bmcl.2011.01.106

Abstract

Continuing studies on tetrahydroquinoline glucocorticoid receptor anti-inflammatory agents lead to the identification of several tetrahydroquinolin-3-yl carbamates that exhibited steroid-like activity in in vitro transrepression assays with reduced transactivation of phosphoenol pyruvate carboxykinase (PEPCK), a key enzyme in the gluconeogenesis pathway.

MeSH terms

Carboxy-Lyases / metabolism*
Enzyme Activation
Quinolines / pharmacology*
Receptors, Glucocorticoid / agonists*

Substances

Quinolines
Receptors, Glucocorticoid
1,2,3,4-tetrahydroquinoline
Carboxy-Lyases