Discovery of Mk-4409, A Novel Oxazole Faah Inhibitor for the Treatment of Inflammatory and Neuropathic Pain
ACS medicinal chemistry letters(2014)
摘要
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.
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关键词
Fatty acid amide hydrolase,FAAH,oxazole,pyrazole,neuropathic pain,inflammatory pain,MK-4409,enzyme,inhibitor,CNS
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