Discovery of MK-4409, a novel oxazole FAAH inhibitor for the treatment of inflammatory and neuropathic pain

Harry R. Chobanian, Yan Guo, Ping Liu, Marc D. Chioda, Selena Fung, Thomas J. Lanza, Linda Chang, Raman K. Bakshi, James P. Dellureficio, Qingmei Hong, Mark McLaughlin, Kevin M. Belyk, Shane W. Krska, Amanda K. Makarewicz, Elliot J. Martel, Joseph F. Leone, Lisa Frey, Bindhu Karanam, Maria Madeira, Raul AlvaroJoyce Shuman, Gino Salituro, Jenna L. Terebetski, Nina Jochnowitz, Shruti Mistry, Erin McGowan, Richard Hajdu, Mark Rosenbach, Catherine Abbadie, Jessica P. Alexander, Lin Lin Shiao, Kathleen M. Sullivan, Ravi P. Nargund, Matthew J. Wyvratt, Linus S. Lin, Robert J. Devita

Research output: Contribution to journalArticlepeer-review

35 Scopus citations

Abstract

We report herein the identification of MK-4409, a potent and selective fatty acid amide hydrolase (FAAH) inhibitor. Starting from a high throughput screening (HTS) hit, medicinal chemistry efforts focused on optimizing of FAAH inhibition in vitro potency, improving the pharmacokinetic (PK) profile, and increasing in vivo efficacy in rodent inflammatory and neuropathic pain assays.

Original languageEnglish
Pages (from-to)717-721
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume5
Issue number6
DOIs
StatePublished - 12 Jun 2014
Externally publishedYes

Keywords

  • CNS
  • FAAH
  • Fatty acid amide hydrolase
  • MK-4409
  • enzyme
  • inflammatory pain
  • inhibitor
  • neuropathic pain
  • oxazole
  • pyrazole

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