Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain

ACS Medicinal Chemistry Letters
2014.0

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.

Knowledge Graph

Similar Paper

Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain
ACS Medicinal Chemistry Letters 2014.0
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): Identification of phenmedipham and amperozide as FAAH inhibitors
Bioorganic & Medicinal Chemistry Letters 2009.0
Design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors
Bioorganic & Medicinal Chemistry 2014.0
Novel inhibitors of fatty acid amide hydrolase
Bioorganic & Medicinal Chemistry Letters 2007.0
Discovery and Development of Fatty Acid Amide Hydrolase (FAAH) Inhibitors
Journal of Medicinal Chemistry 2008.0
Synthesis and Evaluation of Paracetamol Esters As Novel Fatty Acid Amide Hydrolase Inhibitors
Journal of Medicinal Chemistry 2010.0
Reversible Competitive α-Ketoheterocycle Inhibitors of Fatty Acid Amide Hydrolase Containing Additional Conformational Constraints in the Acyl Side Chain: Orally Active, Long-Acting Analgesics
Journal of Medicinal Chemistry 2011.0
A novel monoacylglycerol lipase inhibitor with analgesic and anti-inflammatory activity
Bioorganic & Medicinal Chemistry Letters 2008.0
New FAAH inhibitors based on 3-carboxamido-5-aryl-isoxazole scaffold that protect against experimental colitis
Bioorganic & Medicinal Chemistry 2011.0
1-Heteroarylpropan-2-ones as inhibitors of fatty acid amide hydrolase: Studies on structure-activity relationships and metabolic stability
Bioorganic & Medicinal Chemistry 2017.0