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.
Steven L Roach  1 ,  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
Affiliations
  • 1. Discovery Research, Ligand Pharmaceuticals, La Jolla, CA 92037, USA. [email protected]
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.