2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents
摘要:
Herein we describe a series of potent and selective PPARγ agonists with moderate PPARα affinity and little to no affinity for other nuclear receptors. In vivo studies in a NIDDM animal model (ZDF rat) showed that these compounds are efficacious at low doses in glucose normalization and plasma triglyceride reduction. Compound 1b ( LY519818) was selected from our SAR studies to be advanced to clinical evaluation for the treatment of type II diabetes.
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DOI:
10.1016/j.bmcl.2004.10.042
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年份:
2005
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