203 articles for thisTarget
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Design, Synthesis, Structure-Activity Relationship Studies, and Three-Dimensional Quantitative Structure-Activity Relationship (3D-QSAR) Modeling of a Series of O-Biphenyl Carbamates as Dual Modulators of Dopamine D3 Receptor and Fatty Acid Amide Hydrolase.
Universit£
1-Heteroarylpropan-2-ones as inhibitors of fatty acid amide hydrolase: Studies on structure-activity relationships and metabolic stability.
University of M£Nster
Fatty Acid Amide Hydrolase (FAAH), Acetylcholinesterase (AChE), and Butyrylcholinesterase (BuChE): Networked Targets for the Development of Carbamates as Potential Anti-Alzheimer's Disease Agents.
Alma Mater Studiorum-University of Bologna
The SAR of brain penetration for a series of heteroaryl urea FAAH inhibitors.
Janssen Pharmaceutical Companies of Johnson & Johnson
Piperidinyl thiazole isoxazolines: A new series of highly potent, slowly reversible FAAH inhibitors with analgesic properties.
E.I. Du Pont De Nemours
Development and Pharmacological Characterization of Selective Blockers of 2-Arachidonoyl Glycerol Degradation with Efficacy in Rodent Models of Multiple Sclerosis and Pain.
University of Siena
Potent multitarget FAAH-COX inhibitors: Design and structure-activity relationship studies.
Fondazione Istituto Italiano Di Tecnologia
Revisiting 1,3,4-Oxadiazol-2-ones: Utilization in the Development of ABHD6 Inhibitors.
University of Eastern Finland
Piperazine and piperidine carboxamides and carbamates as inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).
University of Eastern Finland
Pyrazole phenylcyclohexylcarbamates as inhibitors of human fatty acid amide hydrolases (FAAH).
Universit£
Structure-affinity relationships and pharmacological characterization of new alkyl-resorcinol cannabinoid receptor ligands: Identification of a dual cannabinoid receptor/TRPA1 channel agonist.
Universit£
Discovery libraries targeting the major enzyme classes: the serine hydrolases.
The Scripps Research Institute
Identification of endocannabinoid system-modulating N-alkylamides from Heliopsis helianthoides var. scabra and Lepidium meyenii.
University of Szeged
Inhibition of FAAH, TRPV1, and COX2 by NSAID-serotonin conjugates.
Roseman University of Health Sciences
Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain.
Merck Research Laboratories
a-Ketoheterocycle inhibitors of fatty acid amide hydrolase: exploration of conformational constraints in the acyl side chain.
The Scripps Research Institute
Design, synthesis, and characterization ofa-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase.
The Scripps Research Institute
1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase.
Janssen Pharmaceutical Companies of Johnson & Johnson
Switching cannabinoid response from CB(2) agonists to FAAH inhibitors.
University of Lille
Design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors.
Takeda Pharmaceutical
Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty acid amide hydrolase.
Janssen Research and Development
Chiral 1,3,4-oxadiazol-2-ones as highly selective FAAH inhibitors.
University of Eastern Finland
Macamides and their synthetic analogs: evaluation of in vitro FAAH inhibition.
Mcphs University
Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors.
Fondazione Istituto Italiano Di Tecnologia
Development and characterization of a promising fluorine-18 labelled radiopharmaceutical for in vivo imaging of fatty acid amide hydrolase.
Centre For Addiction and Mental Health
Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase.
Merck Research Laboratories
Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: modulation at the N-portion and distal phenyl ring.
Sapienza University of Rome
(4-Phenoxyphenyl)tetrazolecarboxamides and related compounds as dual inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).
University of M£Nster
Identification of a novel arylpiperazine scaffold for fatty acid amide hydrolase inhibition with improved drug disposition properties.
Universit£
Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors.
Takeda Pharmaceutical
An unprecedented reversible mode of action ofß-lactams for the inhibition of human fatty acid amide hydrolase (hFAAH).
Universit£
Radiosynthesis and evaluation of [¹¹C-carbonyl]-labeled carbamates as fatty acid amide hydrolase radiotracers for positron emission tomography.
Centre For Addiction and Mental Health
Tetrahydro-ß-carboline derivatives targeting fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channels.
Sapienza University of Rome
Biphenyl-3-yl alkylcarbamates as fatty acid amide hydrolase (FAAH) inhibitors: steric effects of N-alkyl chain on rat plasma and liver stability.
Universit£
Bis(dialkylaminethiocarbonyl)disulfides as potent and selective monoglyceride lipase inhibitors.
Universite Catholique De Louvain
Synthesis, in vitro and in vivo evaluation, and radiolabeling of aryl anandamide analogues as candidate radioligands for in vivo imaging of fatty acid amide hydrolase in the brain.
Ghent University
Synthesis of 61-bis(1-adamantylcarbamoyl)-1,2-methano[60]fullerene and its antagonistic effect on haloperidol-induced catalepsy in mice.
Kyushu University
Heteroaryl urea inhibitors of fatty acid amide hydrolase: structure-mutagenicity relationships for arylamine metabolites.
Janssen Research and Development
Synopsis of some recent tactical application of bioisosteres in drug design.
Bristol-Myers Squibb Pharmaceutical Research and Development
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
Astrazeneca
Identification and characterization of carprofen as a multitarget fatty acid amide hydrolase/cyclooxygenase inhibitor.
Istituto Italiano Di Tecnologia
Discovery of potent inhibitors of human and mouse fatty acid amide hydrolases.
Universit£
Aryl Piperazinyl Ureas as Inhibitors of Fatty Acid Amide Hydrolase (FAAH) in Rat, Dog, and Primate.
TBA
Development and characterization of endocannabinoid hydrolases FAAH and MAGL inhibitors bearing a benzotriazol-1-yl carboxamide scaffold.
Sapienza University of Rome
Synthesis and pharmacological evaluation of 2,4-dinitroaryldithiocarbamate derivatives as novel monoacylglycerol lipase inhibitors.
Universit£
SAR and LC/MS studies ofß-lactamic inhibitors of human fatty acid amide hydrolase (hFAAH): evidence of a nonhydrolytic process.
Universit£
Structure-activity relationship of a new series of reversible dual monoacylglycerol lipase/fatty acid amide hydrolase inhibitors.
Universidad Complutense De Madrid
Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor.
Pfizer
Discovery and development of fatty acid amide hydrolase (FAAH) inhibitors.
Johnson & Johnson Pharmaceutical Research and Development
Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profiling.
The Scripps Research Institute
Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase.
Institute For Chemical Biology
New tetrazole-based selective anandamide uptake inhibitors.
Sapienza University of Rome
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Johnson & Johnson Pharmaceutical Research & Development
Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.
The Scripps Research Institute
Influence of sulfur oxidation state and steric bulk upon trifluoromethyl ketone (TFK) binding kinetics to carboxylesterases and fatty acid amide hydrolase (FAAH).
University of California
Novel ketooxazole based inhibitors of fatty acid amide hydrolase (FAAH).
Johnson & Johnson Pharmaceutical Research and Development
Design, synthesis, binding, and molecular modeling studies of new potent ligands of cannabinoid receptors.
Universit£
Design, synthesis, and binding studies of new potent ligands of cannabinoid receptors.
Universit£
Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase.
The Scripps Research Institute
New metabolically stable fatty acid amide ligands of cannabinoid receptors: Synthesis and receptor affinity studies.
Institute of Biomolecular Chemistry
The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications.
Universit£
Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: comparison with effects on fatty acid amidohydrolase.
Universidad Complutense
Fatty acid amide hydrolase inhibitors. 3: tetra-substituted azetidine ureas with in vivo activity.
Vernalis (R&D)
Design, synthesis and evaluation of polar head group containing 2-keto-oxazole inhibitors of FAAH.
Max Planck Institute of Molecular Physiology
Benzisothiazolinone as a useful template for the design of new monoacylglycerol lipase inhibitors: investigation of the target residues and comparison with octhilinone.
Universit£
The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH).
The Scripps Research Institute
New FAAH inhibitors based on 3-carboxamido-5-aryl-isoxazole scaffold that protect against experimental colitis.
University of Lille
Reversible competitivea-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics.
The Scripps Research Institute
Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.
Amgen
Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects.
The Scripps Research Institute
Activation of the endocannabinoid system by organophosphorus nerve agents.
University of California
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands.
Sapienza University of Rome
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.
Renovis
Oxime carbamate--discovery of a series of novel FAAH inhibitors.
Bristol-Myers Squibb Research & Development
1-Indol-1-yl-propan-2-ones and related heterocyclic compounds as dual inhibitors of cytosolic phospholipase A(2)alpha and fatty acid amide hydrolase.
University of M£Nster
Synthesis and evaluation of paracetamol esters as novel fatty acid amide hydrolase inhibitors.
University of Cagliari
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
The Scripps Research Institute
X-ray crystallographic analysis of alpha-ketoheterocycle inhibitors bound to a humanized variant of fatty acid amide hydrolase.
The Scripps Research Institute
Synthesis and in vitro evaluation of N-substituted maleimide derivatives as selective monoglyceride lipase inhibitors.
Louvain Drug Research Institute
beta-Lactams derived from a carbapenem chiron are selective inhibitors of human fatty acid amide hydrolase versus human monoacylglycerol lipase.
Universite Catholique De Louvain
Chiral 3-(4,5-dihydrooxazol-2-yl)phenyl alkylcarbamates as novel FAAH inhibitors: Insight into FAAH enantioselectivity by molecular docking and interaction fields.
Helsinki University of Technology
Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas.
Vernalis (R&D)
The synthesis and biological evaluation of para-substituted phenolic N-alkyl carbamates as endocannabinoid hydrolyzing enzyme inhibitors.
University of Kuopio
Radiosynthesis, in vitro and in vivo evaluation of 123I-labeled anandamide analogues for mapping brain FAAH.
Ghent University
Tetrahydrolipstatin analogues as modulators of endocannabinoid 2-arachidonoylglycerol metabolism.
Sapienza University of Rome
Monoacylglycerol lipase regulates 2-arachidonoylglycerol action and arachidonic acid levels.
University of California
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
Johnson & Johnson Pharmaceutical Research and Development
Correlation of inhibitor effects on enzyme activity and thermal stability for the integral membrane protein fatty acid amide hydrolase.
The Scripps Research Institute
Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase.
The Scripps Research Institute
Synthesis and quantitative structure-activity relationship of fatty acid amide hydrolase inhibitors: modulation at the N-portion of biphenyl-3-yl alkylcarbamates.
Università
Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation.
Sapienza University of Rome
Structure-activity relationship of a series of inhibitors of monoacylglycerol hydrolysis--comparison with effects upon fatty acid amide hydrolase.
Universidad Complutense
Design, synthesis, and in vitro evaluation of carbamate derivatives of 2-benzoxazolyl- and 2-benzothiazolyl-(3-hydroxyphenyl)-methanones as novel fatty acid amide hydrolase inhibitors.
Helsinki University of Technology
Fatty acid amide hydrolase inhibitors from virtual screening of the endocannabinoid system.
University of Kuopio
Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.
Lanzhou University
Reversible Monoacylglycerol Lipase Inhibitors: Discovery of a New Class of Benzylpiperidine Derivatives.
University of Pisa
Development of the first potential covalent inhibitors of anandamide cellular uptake.
Institute of Biomolecular Chemistry
Design and synthesis of endocannabinoid enzyme inhibitors for ocular indications.
Liberty University
Synthesis and evaluation of dual fatty acid amide hydrolase-monoacylglycerol lipase inhibition and antinociceptive activities of 4-methylsulfonylaniline-derived semicarbazones.
Indian Institute of Technology (Banaras Hindu University)
Advancements in the development of multi-target directed ligands for the treatment of Alzheimer's disease.
Central University of Punjab
Structure-based design of novel donepezil-like hybrids for a multi-target approach to the therapy of Alzheimer's disease.
University of Bari Aldo Moro
Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics.
The Scripps Research Institute
Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity.
The Scripps Research Institute
Further exploration of the structure-activity relationship of dual soluble epoxide hydrolase/fatty acid amide hydrolase inhibitors.
California State University
Heterocyclic sulfoxide and sulfone inhibitors of fatty acid amide hydrolase.
The Scripps Research Institute
Cyclohexylcarbamic acid 3'- or 4'-substituted biphenyl-3-yl esters as fatty acid amide hydrolase inhibitors: synthesis, quantitative structure-activity relationships, and molecular modeling studies.
Università
Arachidonylsulfonyl derivatives as cannabinoid CB1 receptor and fatty acid amide hydrolase inhibitors.
University of California
Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2
Takeda Pharmaceutical
Hemisynthesis and preliminary evaluation of novel endocannabinoid analogues.
Umr Cnrs 5074
Design, synthesis, and structure-activity relationships of alkylcarbamic acid aryl esters, a new class of fatty acid amide hydrolase inhibitors.
Università
Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.
University of Pisa
Heteroarylureas with fused bicyclic diamine cores as inhibitors of fatty acid amide hydrolase.
Janssen Pharmaceutical Companies of Johnson & Johnson
The endocannabinoid system dual-target ligand N-cycloheptyl-1,2-dihydro-5-bromo-1-(4-fluorobenzyl)-6-methyl-2-oxo-pyridine-3-carboxamide improves disease severity in a mouse model of multiple sclerosis.
University of Pisa
Oxygenated metabolites of anandamide and 2-arachidonoylglycerol: conformational analysis and interaction with cannabinoid receptors, membrane transporter, and fatty acid amide hydrolase.
Utrecht University
A perspective review on fatty acid amide hydrolase (FAAH) inhibitors as potential therapeutic agents.
Assam University (A Central University)
Structural Optimization of 4-Chlorobenzoylpiperidine Derivatives for the Development of Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
University of Pisa
The discovery of diazetidinyl diamides as potent and reversible inhibitors of monoacylglycerol lipase (MAGL).
Janssen Research & Development
The discovery of azetidine-piperazine di-amides as potent, selective and reversible monoacylglycerol lipase (MAGL) inhibitors.
Janssen Research & Development
alpha-Keto heterocycle inhibitors of fatty acid amide hydrolase: carbonyl group modification and alpha-substitution.
The Scripps Research Institute
Discovery of heterocyclic carbohydrazide derivatives as novel selective fatty acid amide hydrolase inhibitors: design, synthesis and anti-neuroinflammatory evaluation.
China Pharmaceutical University
Discovery of Aryl Formyl Piperidine Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase Inhibitors.
China Pharmaceutical University
Design and synthesis of cyanamides as potent and selective N-acylethanolamine acid amidase inhibitors.
Northeastern University
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor.
University of Pisa
Structure-Activity Relationships of Fish Oil Derivatives with Antiallergic Activity in Vitro and in Vivo.
Ehime University
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.
Palack£
Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems.
University of Siena
Synthesis and evaluation of potent and selective MGL inhibitors as a glaucoma treatment.
Mak Scientific
Tetrazolylpropan-2-ones as inhibitors of fatty acid amide hydrolase: Studies on structure-activity relationships and metabolic stability.
University of M£Nster
Trifluoromethyl ketone inhibitors of fatty acid amide hydrolase: a probe of structural and conformational features contributing to inhibition.
Scripps Research Institute
Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model.
Advinus Therapeutics
Piperidine and piperazine inhibitors of fatty acid amide hydrolase targeting excitotoxic pathology.
Northeastern University
Benzisothiazolinone Derivatives as Potent Allosteric Monoacylglycerol Lipase Inhibitors That Functionally Mimic Sulfenylation of Regulatory Cysteines.
Universit£
An endogenous sleep-inducing compound is a novel competitive inhibitor of fatty acid amide hydrolase.
Institute For Chemical Biology
Lead Optimization of Benzoxazolone Carboxamides as Orally Bioavailable and CNS Penetrant Acid Ceramidase Inhibitors.
University of Illinois At Chicago
Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
Julius Maximilian University of W£Rzburg
New Approaches to Cancer Therapy: Combining Fatty Acid Amide Hydrolase (FAAH) Inhibition with Peroxisome Proliferator-Activated Receptors (PPARs) Activation.
Universit£
N-Acyl pyrazoles: Effective and tunable inhibitors of serine hydrolases.
The Scripps Research Institute
Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors.
University of Pisa
Design, Synthesis, and Evaluation of Piperazinyl Pyrrolidin-2-ones as a Novel Series of Reversible Monoacylglycerol Lipase Inhibitors.
Takeda Pharmaceutical
Identification of Bivalent Ligands with Melatonin Receptor Agonist and Fatty Acid Amide Hydrolase (FAAH) Inhibitory Activity That Exhibit Ocular Hypotensive Effect in the Rabbit.
Universit£
Identification and optimization of soluble epoxide hydrolase inhibitors with dual potency towards fatty acid amide hydrolase.
University of California Davis
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
University of Pisa
Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors.
Universit£
Polypharmacological profile of 1,2-dihydro-2-oxo-pyridine-3-carboxamides in the endocannabinoid system.
University of Bern
Biological evaluation of pyridone alkaloids on the endocannabinoid system.
University of Bern
Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation.
Pfizer
Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
University of Ferrara
Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase.
Pfizer
Heterodimerization with Its splice variant blocks the ghrelin receptor 1a in a non-signaling conformation: a study with a purified heterodimer assembled into lipid discs.
Université Montpellier 1
Synthesis, biological evaluation, and molecular docking studies of new pyrazol-3-one derivatives with aromatase inhibition activities.
Yueyang Vocational Technical College
The first selective agonist for the neuropeptide YY5 receptor increases food intake in rats.
Federal Institute of Technology of Zurich
Cloning and functional expression of a human Y4 subtype receptor for pancreatic polypeptide, neuropeptide Y, and peptide YY.
Synaptic Pharmaceutical
Expression cloning and pharmacological characterization of a human hippocampal neuropeptide Y/peptide YY Y2 receptor subtype.
Synaptic Pharmaceutical
Cloning and functional expression of a cDNA encoding a human type 2 neuropeptide Y receptor.
Bristol-Myers Squibb
The cloning and chromosomal mapping of two novel human opioid-somatostatin-like receptor genes, GPR7 and GPR8, expressed in discrete areas of the brain.
Addiction Research Foundation
Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes.
Warner-Lambert/Parke-Davis Pharmaceutical Research
Discovery of inducible nitric oxide synthase (iNOS) inhibitor development candidate KD7332, part 1: Identification of a novel, potent, and selective series of quinolinone iNOS dimerization inhibitors that are orally active in rodent pain models.
Kalypsys
Lead identification to generate isoquinolinedione inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment.
Wyeth Research
Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.
Hoffmann-La Roche
Stereospecific synthesis, structure-activity relationship, and oral bioavailability of tetrahydropyrimidin-2-one HIV protease inhibitors.
Dupont Pharmaceuticals