2. Academic Validation
  3. Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase

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

Affiliation

  • 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.

Figures
Products