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

被引：14

作者：

Acerson, Mark J. ^{[2
]}

Fabick, Kimberly M. ^{[1
]}

Wong, Yong ^{[2
]}

Blake, Crystal ^{[1
]}

Lephart, Edwin D. ^{[1
]}

Andrus, Merritt B. ^{[2
]}

机构：

[1] Brigham Young Univ, Dept Physiol, Ctr Neurosci, Provo, UT 84602 USA

[2] Brigham Young Univ, Dept Chem, Provo, UT 84602 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 10期

关键词：

Resveratrol; Polyphenol; Palladium catalysis; Heck coupling; Anti-depressant; TRANS-RESVERATROL; ACID; RATS; BIOAVAILABILITY; HIPPOCAMPUS; INVOLVEMENT; POLYPHENOL; MECHANISMS; EXPRESSION; ESTROGEN;

D O I：

10.1016/j.bmcl.2013.03.046

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：2941 / 2944

页数：4

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