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Heteroarylureas with fused bicyclic diamine cores as inhibitors of fatty acid amide hydrolase.

Authors
  • Keith, John M1
  • Jones, William2
  • Pierce, Joan M2
  • Seierstad, Mark2
  • Palmer, James A2
  • Webb, Michael2
  • Karbarz, Mark2
  • Scott, Brian P2
  • Wilson, Sandy J2
  • Luo, Lin2
  • Wennerholm, Michelle2
  • Chang, Leon2
  • Rizzolio, Michele2
  • Rynberg, Raymond2
  • Chaplan, Sandra2
  • Guy Breitenbucher, J2
  • 1 Janssen Pharmaceutical Companies of Johnson & Johnson, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. Electronic address: [email protected]
  • 2 Janssen Pharmaceutical Companies of Johnson & Johnson, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Aug 09, 2020
Volume
30
Issue
20
Pages
127463–127463
Identifiers
DOI: 10.1016/j.bmcl.2020.127463
PMID: 32784090
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

A series of mechanism-based heteroaryl urea fatty acid amide hydrolase (FAAH) inhibitors with fused bicyclic diamine cores is described. In contrast to compounds built around a piperazine core, most of the fused bicyclic diamine bearing analogs prepared exhibited greater potency against rFAAH than the human enzyme. Several compounds equipotent against both species were identified and profiled in vivo. Copyright © 2020 Elsevier Ltd. All rights reserved.

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