Bioorganic & Medicinal Chemistry Letters 2009-11-01

Delta agonist hydroxy bioisosteres: the discovery of 3-((1-benzylpiperidin-4-yl){4-[(diethylamino)carbonyl]phenyl}amino)benzamide with improved delta agonist activity and in vitro metabolic stability.

Andrew M Griffin, William Brown, Christopher Walpole, Martin Coupal, Lynda Adam, Mylene Gosselin, Dominic Salois, Pierre-Emmanuel Morin, Marie Roumi

文献索引：Bioorg. Med. Chem. Lett. 19(21) , 5999-6003, (2009)

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摘要

We have investigated phenol replacements in a series of diaryl amino piperidine delta opioid agonists. From this study we have demonstrated that the hydroxy functional group can be replaced with a primary amide group, giving enhanced activity at the delta receptor, increased selectivity versus mu and kappa as well as improved in vitro metabolic stability.