Fatty acid amide hydrolase inhibitors: a patent review (2009 – 2014)

Multitarget fatty acid amide hydrolase/cyclooxygenase blockade suppresses intestinal inflammation and protects against nonsteroidal anti-inflammatory drug-dependent gastrointestinal damage

(2015) Oscar Sasso et al.   FASEB JOURNAL

Structure of Human N -Acylphosphatidylethanolamine-Hydrolyzing Phospholipase D: Regulation of Fatty Acid Ethanolamide Biosynthesis by Bile Acids

(2015) Paola Magotti et al.   STRUCTURE

1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase

(2014) John M. Keith et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty acid amide hydrolase

(2014) John M. Keith et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2014) Harry R. Chobanian et al.   ACS Medicinal Chemistry Letters

Latest advances in the discovery of fatty acid amide hydrolase inhibitors

(2013) Tiziana Bisogno et al.   Expert Opinion on Drug Discovery

Quantum Mechanics/Molecular Mechanics Modeling of Fatty Acid Amide Hydrolase Reactivation Distinguishes Substrate from Irreversible Covalent Inhibitors

(2013) Alessio Lodola et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase

(2013) Ping Liu et al.   ACS Medicinal Chemistry Letters

Discovery of Potent Inhibitors of Human and Mouse Fatty Acid Amide Hydrolases

(2012) Stefania Butini et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Binding Site for Nonsteroidal Anti-inflammatory Drugs in Fatty Acid Amide Hydrolase

(2012) Laura Bertolacci et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The pharmacological landscape and therapeutic potential of serine hydrolases

(2012) Daniel A. Bachovchin et al.   NATURE REVIEWS DRUG DISCOVERY

Inhibitors of endocannabinoid breakdown for pain: Not so FA(AH)cile, after all

(2012) Vincenzo Di Marzo   PAIN

Discovery of potent, non-carbonyl inhibitors of fatty acid amide hydrolase (FAAH)

(2012) Sumithra Gowlugari et al.   MedChemComm

Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 1: Identification of 7-azaspiro[3.5]nonane and 1-oxa-8-azaspiro[4.5]decane as lead scaffolds

(2011) Marvin J. Meyers et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 2. Discovery of 7-azaspiro[3.5]nonane urea PF-04862853, an orally efficacious inhibitor of fatty acid amide hydrolase (FAAH) for pain

(2011) Marvin J. Meyers et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH)

(2011) Katerina Otrubova et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Fatty acid amide hydrolase inhibitors. 3: Tetra-substituted azetidine ureas with in vivo activity

(2011) Stephen D. Roughley et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Fatty Acid-binding Proteins TransportN-Acylethanolamines to Nuclear Receptors and Are Targets of Endocannabinoid Transport Inhibitors

(2011) Martin Kaczocha et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Covalent Inhibitors of Fatty Acid Amide Hydrolase: A Rationale for the Activity of Piperidine and Piperazine Aryl Ureas

(2011) Giulia Palermo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Reversible Competitive α-Ketoheterocycle Inhibitors of Fatty Acid Amide Hydrolase Containing Additional Conformational Constraints in the Acyl Side Chain: Orally Active, Long-Acting Analgesics

(2011) Cyrine Ezzili et al.   JOURNAL OF MEDICINAL CHEMISTRY

A catalytically silent FAAH-1 variant drives anandamide transport in neurons

(2011) Jin Fu et al.   NATURE NEUROSCIENCE

Discovery and molecular basis of potent noncovalent inhibitors of fatty acid amide hydrolase (FAAH)

(2011) X. Min et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Supply and demand for endocannabinoids

(2011) Bradley E. Alger et al.   TRENDS IN NEUROSCIENCES

Enzymological studies on the biosynthesis of N-acylethanolamines

(2010) Natsuo Ueda et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Enol Carbamates as Inhibitors of Fatty Acid Amide Hydrolase (FAAH) Endowed with High Selectivity for FAAH over the Other Targets of the Endocannabinoid System

(2010) Sonia Gattinoni et al.   ChemMedChem

Endocannabinoid biosynthesis and inactivation, from simple to complex

(2010) Giulio G. Muccioli   DRUG DISCOVERY TODAY

Anandamide suppresses pain initiation through a peripheral endocannabinoid mechanism

(2010) Jason R Clapper et al.   NATURE NEUROSCIENCE

N-acylethanolamine metabolism with special reference to N-acylethanolamine-hydrolyzing acid amidase (NAAA)

(2010) Natsuo Ueda et al.   PROGRESS IN LIPID RESEARCH

Insights into the mechanism and inhibition of fatty acid amide hydrolase from quantum mechanics/molecular mechanics (QM/MM) modelling

(2009) Alessio Lodola et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

1-Indol-1-yl-propan-2-ones and related heterocyclic compounds as dual inhibitors of cytosolic phospholipase A2α and fatty acid amide hydrolase

(2009) Laura Forster et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas

(2009) Terance Hart et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery and Characterization of a Highly Selective FAAH Inhibitor that Reduces Inflammatory Pain

(2009) Kay Ahn et al.   CHEMISTRY & BIOLOGY

Structure-Property Relationships of a Class of Carbamate-Based Fatty Acid Amide Hydrolase (FAAH) Inhibitors: Chemical and Biological Stability

(2009) Federica Vacondio et al.   ChemMedChem

A Second Generation of Carbamate-Based Fatty Acid Amide Hydrolase Inhibitors with Improved Activity in vivo

(2009) Jason R. Clapper et al.   ChemMedChem

Binding and Inactivation Mechanism of a Humanized Fatty Acid Amide Hydrolase by α-Ketoheterocycle Inhibitors Revealed from Cocrystal Structures

(2009) Mauro Mileni et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Selective N-acylethanolamine-hydrolyzing acid amidase inhibition reveals a key role for endogenous palmitoylethanolamide in inflammation

(2009) C. Solorzano et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Biochemical and Biological Properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a Mechanism-Based Inhibitor of Fatty Acid Amide Hydrolase

(2008) Mark J. Karbarz et al.   ANESTHESIA AND ANALGESIA

Fatty Acid Amide Hydrolase Inhibition Heightens Anandamide Signaling Without Producing Reinforcing Effects in Primates

(2008) Zuzana Justinova et al.   BIOLOGICAL PSYCHIATRY

Enzymatic Pathways That Regulate Endocannabinoid Signaling in the Nervous System

(2008) Kay Ahn et al.   CHEMICAL REVIEWS

Discovery of Boronic Acids as Novel and Potent Inhibitors of Fatty Acid Amide Hydrolase

(2008) Anna Minkkilä et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery and Development of Fatty Acid Amide Hydrolase (FAAH) Inhibitors

(2008) Mark Seierstad et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting the endocannabinoid system: to enhance or reduce?

(2008) Vincenzo Di Marzo   NATURE REVIEWS DRUG DISCOVERY