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Bioorg Med Chem Lett. 2008 Sep 1;18(17):4838-43. doi: 10.1016/j.bmcl.2008.07.081. Epub 2008 Jul 25.

Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.

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  • 1Johnson & Johnson Pharmaceutical Research and Development, LLC, 3210 Merryfield Row, San Diego, CA 92121, USA.


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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