Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371413 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
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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Authors
Andrew R. Hudson, 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,