2. Academic Validation
  3. Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation

Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation

  • Bioorg Med Chem Lett. 2011 Mar 15;21(6):1654-7. doi: 10.1016/j.bmcl.2011.01.104.
Andrew R Hudson 1,  Robert I Higuchi,  Steven L Roach,  Lino J Valdez,  Mark E Adams,  Angie Vassar,  Deepa Rungta,  Peter M Syka,  Dale E Mais,  Keith B Marschke,  Lin Zhi
Affiliations

Affiliation

  • 1 Discovery Research, Ligand Pharmaceuticals, La Jolla, CA 92037, USA. andyrhudson@gmail.com
PMID: 21324689 DOI: 10.1016/j.bmcl.2011.01.104
Abstract

Continuing studies based on dihydroquinoline Glucocorticoid Receptor agonists lead to the discovery of a series of C4-oxime analogs. Representative compounds exhibited potent transrepression activity with minimal transactivation of phosphoenolpyruvate caboxykinase (PEPCK), a key protein in the gluconeogenesis pathway. These compounds represent promising leads in identifying GR agonists with high anti-inflammatory activity and attenuated potential for glucose elevation.

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