ArticleJournal of medicinal chemistry2013
Discovery and optimization of piperidyl-1,2,3-triazole ureas as potent, selective, and in vivo-active inhibitors of α/β-hydrolase domain containing 6 (ABHD6).
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.
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Who cites it
40 citing papers in PubMed, 88 citations in OpenAlex.
- Design, Synthesis and Antiproliferative Activity Studies of Novel 1,2,3-Triazole-Urea Hybrids.Drug design, development and therapy · 2025Article
- P2XBritish journal of pharmacology · 2024Article
- Development of Oxadiazolone Activity-Based Probes Targeting FphE for Specific Detection ofbioRxiv : the preprint server for biology · 2023Article
- Firefly luciferin methyl ester illuminates the activity of multiple serine hydrolases.Chemical communications (Cambridge, England) · 2023Article
- The serine hydrolase ABHD6 controls survival and thermally induced seizures in a mouse model of Dravet syndrome.Neurobiology of disease · 2023Article
- Identification of cell wall synthesis inhibitors active against Mycobacterium tuberculosis by competitive activity-based protein profiling.Cell chemical biology · 2022Article
- ABHD6 Controls Amphetamine-Stimulated Hyperlocomotion: Involvement of CBCannabis and cannabinoid research · 2022Article
- Reactive chemistry for covalent probe and therapeutic development.Trends in pharmacological sciences · 2022Review
- ABHD6 Inhibition Rescues a Sex-Dependent Deficit in Motor Coordination in The HdhQ200/200 Mouse Model of Huntington's Disease.Journal of neurology and neurological disorders · 2021Article
- α/β-Hydrolase Domain (ABHD) Inhibitors as New Potential Therapeutic Options against Lipid-Related Diseases.Journal of medicinal chemistry · 2021Review
- The endocannabinoid system - current implications for drug development.Journal of internal medicine · 2021Review
- Development and biological applications of sulfur-triazole exchange (SuTEx) chemistry.RSC chemical biology · 2021Article
- Carnitine palmitoyltransferase 1C negatively regulates the endocannabinoid hydrolase ABHD6 in mice, depending on nutritional status.British journal of pharmacology · 2021Article
- Piperidine based 1,2,3-triazolylacetamide derivatives induce cell cycle arrest and apoptotic cell death inJournal of advanced research · 2021Article
- Identification of SARS-CoV-2 Cell Entry Inhibitors by Drug Repurposing UsingFrontiers in immunology · 2020Article
- Structure Kinetics Relationships and Molecular Dynamics Show Crucial Role for Heterocycle Leaving Group in Irreversible Diacylglycerol Lipase Inhibitors.Journal of medicinal chemistry · 2019Article
- Biochemical and microbiological evaluation ofMedChemComm · 2019Article
- Lipid-metabolizing serine hydrolases in the mammalian central nervous system: endocannabinoids and beyond.Biochimica et biophysica acta. Molecular and cell biology of lipids · 2019Review
- Fluorescent Triazole Urea Activity-Based Probes for the Single-Cell Phenotypic Characterization of Staphylococcus aureus.Angewandte Chemie (International ed. in English) · 2019Article
- N-Acyl pyrazoles: Effective and tunable inhibitors of serine hydrolases.Bioorganic & medicinal chemistry · 2019Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
α/β-Hydrolase domain containing 6 (ABHD6) is a transmembrane serine hydrolase that hydrolyzes the endogenous cannabinoid 2-arachidonoylglycerol (2-AG) to regulate certain forms of cannabinoid receptor-dependent signaling in the nervous system. The full spectrum of ABHD6 metabolic activities and functions is currently unknown and would benefit from selective, in vivo-active inhibitors. Here, we report the development and characterization of an advanced series of irreversible (2-substituted)-piperidyl-1,2,3-triazole urea inhibitors of ABHD6, including compounds KT182 and KT203, which show exceptional potency and selectivity in cells (<5 nM) and, at equivalent doses in mice (1 mg kg(-1)), act as systemic and peripherally restricted ABHD6 inhibitors, respectively. We also describe an orally bioavailable ABHD6 inhibitor, KT185, that displays excellent selectivity against other brain and liver serine hydrolases in vivo. We thus describe several chemical probes for biological studies of ABHD6, including brain-penetrant and peripherally restricted inhibitors that should prove of value for interrogating ABHD6 function in animal models.
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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.