Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl Moiety

The discovery of diazetidinyl diamides as potent and reversible inhibitors of monoacylglycerol lipase (MAGL)

(2020) Bin Zhu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The discovery of azetidine-piperazine di-amides as potent, selective and reversible monoacylglycerol lipase (MAGL) inhibitors

(2020) Bin Zhu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

An updated patent review of monoacylglycerol lipase (MAGL) inhibitors (2018-present)

(2020) Giulia Bononi et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor

(2019) Carlotta Granchi et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2019) Ryan M. Wyatt et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation

(2018) Laura A. McAllister et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors

(2018) Mojgan Aghazadeh Tabrizi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders

(2018) Justin S. Cisar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, and evaluation of piperazinyl pyrrolidin-2-ones as a novel series of reversible monoacylglycerol lipase inhibitors

(2018) Jumpei Aida et al.   JOURNAL OF MEDICINAL CHEMISTRY

A patent review of Monoacylglycerol Lipase (MAGL) inhibitors (2013-2017)

(2017) Carlotta Granchi et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase

(2017) Christopher R. Butler et al.   JOURNAL OF MEDICINAL CHEMISTRY

Monoglyceride lipase as a drug target: At the crossroads of arachidonic acid metabolism and endocannabinoid signaling

(2017) Gernot F. Grabner et al.   PHARMACOLOGY & THERAPEUTICS

Kinetic solubility and lipophilicity evaluation connecting formulation technology strategy perspective

(2016) Katsuhiko Yamamoto et al.   JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY

Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors

(2016) Wei Tuo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural Optimization of 4-Chlorobenzoylpiperidine Derivatives for the Development of Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors

(2016) Carlotta Granchi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Crucial Roles of the Endocannabinoid 2-Arachidonoylglycerol in the Suppression of Epileptic Seizures

(2016) Yuki Sugaya et al.   Cell Reports

CNS Drug Design: Balancing Physicochemical Properties for Optimal Brain Exposure

(2015) Zoran Rankovic   JOURNAL OF MEDICINAL CHEMISTRY

A Reversible and Selective Inhibitor of Monoacylglycerol Lipase Ameliorates Multiple Sclerosis

(2014) Gloria Hernández-Torres et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Chemical approaches to therapeutically target the metabolism and signaling of the endocannabinoid 2-AG and eicosanoids

(2014) Rebecca A. Kohnz et al.   CHEMICAL SOCIETY REVIEWS

Design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors

(2013) Mitsunori Kono et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Impact of Physicochemical Profiling for Rational Approach on Drug Discovery

(2013) Shoko Nakashima et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

The pharmacological landscape and therapeutic potential of serine hydrolases

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

The serine hydrolases MAGL, ABHD6 and ABHD12 as guardians of 2-arachidonoylglycerol signalling through cannabinoid receptors

(2011) J. R. Savinainen et al.   Acta Physiologica

Crystal structure of a soluble form of human monoglyceride lipase in complex with an inhibitor at 1.35 Å resolution

(2011) Céline Schalk-Hihi et al.   PROTEIN SCIENCE

Endocannabinoid Hydrolysis Generates Brain Prostaglandins That Promote Neuroinflammation

(2011) D. K. Nomura et al.   SCIENCE

A Medicinal Chemist’s Guide to Molecular Interactions

(2010) Caterina Bissantz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chronic monoacylglycerol lipase blockade causes functional antagonism of the endocannabinoid system

(2010) Joel E Schlosburg et al.   NATURE NEUROSCIENCE

Membrane transporters in drug development

(2010)   NATURE REVIEWS DRUG DISCOVERY

The design of efficient and selective routes to pyridyl analogues of 3-oxo-3,4-dihydro-2H-1,4-(benzothiazine or benzoxazine)-6-carbaldehydes

(2010) Gerald Brooks et al.   TETRAHEDRON LETTERS

Characterization of Monoacylglycerol Lipase Inhibition Reveals Differences in Central and Peripheral Endocannabinoid Metabolism

(2009) Jonathan Z. Long et al.   CHEMISTRY & BIOLOGY

Discovery of Potent and Reversible Monoacylglycerol Lipase Inhibitors

(2009) Alvin R. King et al.   CHEMISTRY & BIOLOGY

Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success

(2009) Frank Lovering et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural Basis for Human Monoglyceride Lipase Inhibition

(2009) T. Bertrand et al.   JOURNAL OF MOLECULAR BIOLOGY

Endocannabinoid-Mediated Control of Synaptic Transmission

(2009) Masanobu Kano et al.   PHYSIOLOGICAL REVIEWS