Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain
ACS Medicinal Chemistry Letters2014Vol. 5(6), pp. 717–721
Citations Over TimeTop 10% of 2014 papers
Harry R. Chobanian, Yan Guo, Ping Liu, Marc 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 Makarewicz, Elliot J. Martel, Joseph F. Leone, Lisa Frey, Bindhu V. Karanam, Maria Madeira, Raúl Álvaro, Joyce B. 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
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.
Related Papers
- → Fatty Acid Amide Hydrolase Inhibitors – Progress and Potential(2011)27 cited
- → S265. Endocannabinoid Metabolism and Alcohol Consumption in Youth: A PET Study With the Fatty Acid Amide Hydrolase Radioligand [11C]CURB(2018)4 cited
- → 51. Investigating Endocannabinoid Mechanisms in Posttraumatic Stress Disorder: Neuroimaging Studies With the Novel Fatty Acid Amide Hydrolase Probe, [11C]CURB(2018)3 cited
- → Next Stop for Fatty Acid Amide Hydrolase Inhibitors, the Clinic?(2020)1 cited
- → fatty acid amide hydrolase 3.5.1.99(2013)1 cited