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.

Abstract:

: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.

journal_name

Bioorg Med Chem Lett

authors

Griffin AM,Brown W,Walpole C,Coupal M,Adam L,Gosselin M,Salois D,Morin PE,Roumi M

doi

10.1016/j.bmcl.2009.09.068

subject

Has Abstract

pub_date

2009-11-01 00:00:00

pages

5999-6003

issue

21

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)01336-5

journal_volume

19

pub_type

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