2. Academic Validation
  3. 1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase

1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase

  • Bioorg Med Chem Lett. 2014 Mar 1;24(5):1280-4. doi: 10.1016/j.bmcl.2014.01.064.
John M Keith 1,  Natalie Hawryluk 2,  Richard L Apodaca 2,  Allison Chambers 2,  Joan M Pierce 2,  Mark Seierstad 2,  James A Palmer 2,  Michael Webb 2,  Mark J Karbarz 2,  Brian P Scott 2,  Sandy J Wilson 2,  Lin Luo 2,  Michelle L Wennerholm 2,  Leon Chang 2,  Michele Rizzolio 2,  Sandra R Chaplan 2,  J Guy Breitenbucher 2
Affiliations

Affiliations

  • 1 Janssen Pharmaceutical Companies of Johnson & Johnson, 3210 Merryfield Row, San Diego, CA 92121, United States. Electronic address: jkeith@its.jnj.com.
  • 2 Janssen Pharmaceutical Companies of Johnson & Johnson, 3210 Merryfield Row, San Diego, CA 92121, United States.
PMID: 24513048 DOI: 10.1016/j.bmcl.2014.01.064
Abstract

A series of 1-aryl-2-(((6-aryl)pyrimidin-4-yl)amino)ethanols have been found to be competitive inhibitors of fatty acid amide hydrolase (FAAH). One member of this class, JNJ-40413269, was found to have excellent pharmacokinetic properties, demonstrated robust central target engagement, and was efficacious in a rat model of neuropathic pain.

Keywords

Analgesia; Crystal structure; Endo-cannabinoids; Enzymes; Fatty acid amide hydrolase (FAAH).

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