ArticleJournal of medicinal chemistry2010
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
Article in Journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 58 citations in OpenAlex.
- Article
- Promising Inhibitors of Endocannabinoid Degrading Enzymes Sharing a Carbamate Scaffold.Mini reviews in medicinal chemistry · 2025Review
- Novel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold.Journal of medicinal chemistry · 2021Article
- Targeting Monoacylglycerol Lipase in Pursuit of Therapies for Neurological and Neurodegenerative Diseases.Molecules (Basel, Switzerland) · 2021Review
- Development of a highly-specificActa pharmaceutica Sinica. B · 2021Article
- Analgesic and Anticancer Activity of Benzoxazole Clubbed 2-Pyrrolidinones as Novel Inhibitors of Monoacylglycerol Lipase.Molecules (Basel, Switzerland) · 2021Article
- Piperazine- and Piperidine-Containing Thiazolo[5,4-Pharmaceuticals (Basel, Switzerland) · 2020Article
- Increasing levels of the endocannabinoid 2-AG is neuroprotective in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine mouse model of Parkinson's disease.Experimental neurology · 2015Article
- Optimization of 1,2,5-thiadiazole carbamates as potent and selective ABHD6 inhibitors.ChemMedChem · 2015Article
- Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase: New Targets for Future Antidepressants.Current neuropharmacology · 2015Review
- Radiosynthesis and ex vivo evaluation of [(11)C-carbonyl]carbamate- and urea-based monoacylglycerol lipase inhibitors.Nuclear medicine and biology · 2014Article
- Chemical modulation of glycerolipid signaling and metabolic pathways.Biochimica et biophysica acta · 2014Review
- A high-throughput, multiplexed assay for superfamily-wide profiling of enzyme activity.Nature chemical biology · 2014Article
- Evaluation of NHS carbamates as a potent and selective class of endocannabinoid hydrolase inhibitors.ACS chemical neuroscience · 2013Article
- Proteome-wide reactivity profiling identifies diverse carbamate chemotypes tuned for serine hydrolase inhibition.ACS chemical biology · 2013Article
- Chemical probes of endocannabinoid metabolism.Pharmacological reviews · 2013Review
- Highly predictive ligand-based pharmacophore and homology models of ABHD6.Chemical biology & drug design · 2013Article
- Monoacylglycerol lipase - a target for drug development?British journal of pharmacology · 2012Review
- Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group that is bioisosteric with endocannabinoid substrates.Chemistry & biology · 2012Article
- O-hydroxyacetamide carbamates as a highly potent and selective class of endocannabinoid hydrolase inhibitors.ACS chemical neuroscience · 2012Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH) are two enzymes from the serine hydrolase superfamily that degrade the endocannabinoids 2-arachidonoylglycerol and anandamide, respectively. We have recently discovered that MAGL and FAAH are both inhibited by carbamates bearing an N-piperidine/piperazine group. Piperidine/piperazine carbamates show excellent in vivo activity, raising brain endocannabinoid levels and producing CB1-dependent behavioral effects in mice, suggesting that they represent a promising class of inhibitors for studying the endogenous functions of MAGL and FAAH. Herein, we disclose a full account of the syntheses, structure-activity relationships, and inhibitory activities of piperidine/piperazine carbamates against members of the serine hydrolase family. These scaffolds can be tuned for MAGL-selective or dual MAGL-FAAH inhibition by the attachment of an appropriately substituted bisarylcarbinol or aryloxybenzyl moiety, respectively, on the piperidine/piperazine ring. Modifications to the piperidine/piperazine ring ablated inhibitory activity, suggesting a strict requirement for a six-membered ring to maintain potency.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.