A new synthesis of 4 '-resveratrol esters and evaluation of the potential for anti-depressant activity

作者:Acerson Mark J; Fabick Kimberly M; Wong Yong; Blake Crystal; Lephart Edwin D; Andrus Merritt B*
来源:Bioorganic & Medicinal Chemistry Letters, 2013, 23(10): 2941-2944.
DOI:10.1016/j.bmcl.2013.03.046

摘要

The 4'-ester analog of the disease preventative resveratrol 1 (RV), 4'-acetyl-RV 2 along with 4'-pivaloate 13 and benzoate 14 RV were synthesized. The previously developed palladium catalyzed decarbonylative Heck coupling was used to assemble the stilbene core together with 3,5-dibenzyl protected phenol intermediates that allowed for efficient coupling and deprotection using boron trifiuoride etherate. Studies with Long-Evans rats were performed to establish safety, toxicity, and behavioral parameters. In addition, the Porsalt forced-swim test was used to demonstrate anti-depressant activity.

  • 出版日期2013-5-15