2. Academic Validation
  3. 4-Piperidin-4-ylidenemethyl-benzamides as δ-opioid receptor agonists for CNS indications: identifying clinical candidates

4-Piperidin-4-ylidenemethyl-benzamides as δ-opioid receptor agonists for CNS indications: identifying clinical candidates

  • Bioorg Med Chem Lett. 2012 Jan 15;22(2):1174-8. doi: 10.1016/j.bmcl.2011.11.089.
Cathy L Dantzman 1,  Megan M King,  Glen E Ernst,  Xia Wang,  John P McCauley Jr,  Donald W Andisik,  Kelly Brush,  Khanh H Bui,  William Frietze,  Valerie Hoesch,  Jay Liu,  William E Palmer,  Nathan Spear,  Thomas J Hudzik,  Steven S Wesolowski
Affiliations

Affiliation

  • 1 AstraZeneca Pharmaceuticals, 1800 Concord Pike, Wilmington, DE 19850, USA.
PMID: 22197137 DOI: 10.1016/j.bmcl.2011.11.089
Abstract

A series of 4-piperidin-4-ylidenemethyl-benzamide δ-opioid receptor agonists is described with an emphasis on balancing the potency, subtype selectivity and in vitro ADME and safety properties. The three sites impacting SAR are substitutions on the aryl group (R(1)), the piperidine nitrogen (R(2)), and the amide (R(3)). Each region contributes to the balance of properties for δ opioid activity and a desirable CNS profile, and two clinical candidates (20 and 24) were advanced.

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