Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase

  • Bioorg Med Chem Lett. 2008 Sep 1;18(17):4838-43. doi: 10.1016/j.bmcl.2008.07.081.
John M Keith  1 ,  Richard Apodaca ,  Wei Xiao ,  Mark Seierstad ,  Kanaka Pattabiraman ,  Jiejun Wu ,  Michael Webb ,  Mark J Karbarz ,  Sean Brown ,  Sandy Wilson ,  Brian Scott ,  Chui-Se Tham ,  Lin Luo ,  James Palmer ,  Michelle Wennerholm ,  Sandra Chaplan ,  J Guy Breitenbucher
Affiliations
  • 1. Johnson & Johnson Pharmaceutical Research and Development, LLC, 3210 Merryfield Row, San Diego, CA 92121, USA.
PMID: 18693015 DOI: 10.1016/j.bmcl.2008.07.081
Abstract

A series of thiadiazolopiperazinyl aryl urea fatty acid amide hydrolase (FAAH) inhibitors is described. The molecules were found to inhibit the enzyme by acting as mechanism-based substrates, forming a covalent bond with Ser241. SAR and PK properties are presented.

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