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.
Keywords: CNS; FAAH; Fatty acid amide hydrolase; MK-4409; enzyme; inflammatory pain; inhibitor; neuropathic pain; oxazole; pyrazole.