Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation
作者: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
DOI:10.1016/j.bmcl.2011.01.104
日期:2011.3
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. (C) 2011 Elsevier Ltd. All rights reserved.