Skip to main content
U.S. Department of Energy
Office of Scientific and Technical Information

Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MA

Journal Article · · J. Med. Chem.

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; INDUSTRY
OSTI ID:
1834911
Journal Information:
J. Med. Chem., Vol. 64, Issue (15)
Country of Publication:
United States
Language:
ENGLISH

References (42)

Endocannabinoid-Mediated Control of Synaptic Transmission January 2009
2-Arachidonoylgylcerol: A Possible Endogenous Cannabinoid Receptor Ligand in Brain October 1995
Evidence That the Cannabinoid CB1 Receptor Is a 2-Arachidonoylglycerol Receptor January 1999
Biochemistry, pharmacology and physiology of 2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand September 2006
A Comprehensive Profile of Brain Enzymes that Hydrolyze the Endocannabinoid 2-Arachidonoylglycerol December 2007
The serine hydrolases MAGL, ABHD6 and ABHD12 as guardians of 2-arachidonoylglycerol signalling through cannabinoid receptors: The three guardians of 2-AG signalling April 2011
The pharmacological landscape and therapeutic potential of serine hydrolases January 2012
cDNA Cloning, Tissue Distribution, and Identification of the Catalytic Triad of Monoglyceride Lipase October 1997
A role for monoglyceride lipase in 2-arachidonoylglycerol inactivation December 2002
Characterization of Monoacylglycerol Lipase Inhibition Reveals Differences in Central and Peripheral Endocannabinoid Metabolism July 2009
Endocannabinoid Hydrolysis Generates Brain Prostaglandins That Promote Neuroinflammation November 2011
Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N -Acylethanolamine Acid Amidase Inhibitors November 2016
An updated patent review of monoacylglycerol lipase (MAGL) inhibitors (2018-present) November 2020
A patent review of Monoacylglycerol Lipase (MAGL) inhibitors (2013-2017) September 2017
Chemical approaches to therapeutically target the metabolism and signaling of the endocannabinoid 2-AG and eicosanoids January 2014
Chemical Probes of Endocannabinoid Metabolism February 2013
Monoglyceride lipase as a drug target: At the crossroads of arachidonic acid metabolism and endocannabinoid signaling July 2017
Crucial Roles of the Endocannabinoid 2-Arachidonoylglycerol in the Suppression of Epileptic Seizures August 2016
Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders August 2018
Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation March 2018
Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase December 2017
Chronic monoacylglycerol lipase blockade causes functional antagonism of the endocannabinoid system August 2010
Design, Synthesis, and Evaluation of Piperazinyl Pyrrolidin-2-ones as a Novel Series of Reversible Monoacylglycerol Lipase Inhibitors September 2018
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor February 2019
Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors January 2018
Structural Optimization of 4-Chlorobenzoylpiperidine Derivatives for the Development of Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors November 2016
A Reversible and Selective Inhibitor of Monoacylglycerol Lipase Ameliorates Multiple Sclerosis October 2014
Pharmacologic Characterization of JNJ-42226314, [1-(4-Fluorophenyl)indol-5-yl]-[3-[4-(thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone, a Reversible, Selective, and Potent Monoacylglycerol Lipase Inhibitor December 2019
The discovery of diazetidinyl diamides as potent and reversible inhibitors of monoacylglycerol lipase (MAGL) June 2020
The discovery of azetidine-piperazine di-amides as potent, selective and reversible monoacylglycerol lipase (MAGL) inhibitors July 2020
Discovery of Potent and Reversible Monoacylglycerol Lipase Inhibitors October 2009
The influence of drug-like concepts on decision-making in medicinal chemistry November 2007
Kinetic solubility and lipophilicity evaluation connecting formulation technology strategy perspective June 2016
Structural Basis for Human Monoglyceride Lipase Inhibition February 2010
Crystal structure of a soluble form of human monoglyceride lipase in complex with an inhibitor at 1.35 Å resolution: Crystal Structure of Monoglyceride Lipase March 2011
A Medicinal Chemist’s Guide to Molecular Interactions July 2010
CNS Drug Design: Balancing Physicochemical Properties for Optimal Brain Exposure January 2015
Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success November 2009
Impact of Physicochemical Profiling for Rational Approach on Drug Discovery January 2013
Design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors February 2014
The design of efficient and selective routes to pyridyl analogues of 3-oxo-3,4-dihydro-2H-1,4-(benzothiazine or benzoxazine)-6-carbaldehydes September 2010
Establishment and Characterization of the Transformants Stably-Expressing MDR1 Derived from Various Animal Species in LLC-PK1 June 2006