Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain.
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ABSTRACT:
SUBMITTER: Chobanian HR
PROVIDER: S-EPMC4060928 | biostudies-literature | 2014 Jun
REPOSITORIES: biostudies-literature
Publications
Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain.
Chobanian Harry R HR Guo Yan Y Liu Ping P Chioda Marc D MD Fung Selena S Lanza Thomas J TJ Chang Linda L Bakshi Raman K RK Dellureficio James P JP Hong Qingmei Q McLaughlin Mark M Belyk Kevin M KM Krska Shane W SW Makarewicz Amanda K AK Martel Elliot J EJ Leone Joseph F JF Frey Lisa L Karanam Bindhu B Madeira Maria M Alvaro Raul R Shuman Joyce J Salituro Gino G Terebetski Jenna L JL Jochnowitz Nina N Mistry Shruti S McGowan Erin E Hajdu Richard R Rosenbach Mark M Abbadie Catherine C Alexander Jessica P JP Shiao Lin-Lin LL Sullivan Kathleen M KM Nargund Ravi P RP Wyvratt Matthew J MJ Lin Linus S LS DeVita Robert J RJ
ACS medicinal chemistry letters 20140410 6
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. ...[more]
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