ArticleAngewandte Chemie (International ed. in English)2016
Second-Generation Non-Covalent NAAA Inhibitors are Protective in a Model of Multiple Sclerosis.
Article in Angewandte Chemie (International ed. in English), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
21 citing papers in PubMed, 49 citations in OpenAlex.
- Dose-dependent effects of oral cannabidiol and delta-9-tetrahydrocannabinol on serum anandamide and related N-acylethanolamines in healthy volunteers.BMJ mental health · 2024Trial
- The Role of Lipid Alteration in Multiple Sclerosis.International journal of molecular sciences · 2026Review
- Article
- Synthesis of piperazine-based benzimidazole derivatives as potent urease inhibitors and molecular docking studies.Scientific reports · 2025Article
- Exploring the Potential of Coumarin Derivatives on Serotonin Receptors 5-HTInternational journal of molecular sciences · 2025Article
- New bis-piperazine derivatives: synthesis, characterization (IR, NMR), gamma-ray absorption, antimicrobial activity, molecular docking and dynamics study.Turkish journal of chemistry · 2025Article
- The Benzoylpiperidine Fragment as a Privileged Structure in Medicinal Chemistry: A Comprehensive Review.Molecules (Basel, Switzerland) · 2024Review
- Utility of 2-Chloro-ACS omega · 2024Article
- NAAA-regulated lipid signaling in monocytes controls the induction of hyperalgesic priming in mice.Nature communications · 2024Article
- Goods and Bads of the Endocannabinoid System as a Therapeutic Target: Lessons Learned after 30 Years.Pharmacological reviews · 2023Review
- Targeting NAAA counters dopamine neuron loss and symptom progression in mouse models of parkinsonism.Pharmacological research · 2022Article
- Piperazine skeleton in the structural modification of natural products: a review.Journal of enzyme inhibition and medicinal chemistry · 2021Review
- Discovery and SAR Evolution of Pyrazole Azabicyclo[3.2.1]octane Sulfonamides as a Novel Class of Non-CovalentJournal of medicinal chemistry · 2021Article
- Neuroprotective and Immunomodulatory Action of the Endocannabinoid System under Neuroinflammation.International journal of molecular sciences · 2021Review
- Natural Potent NAAA Inhibitor Atractylodin Counteracts LPS-Induced Microglial Activation.Frontiers in pharmacology · 2020Article
- Article
- Synthesis, biological evaluation, and structure activity relationship (SAR) study of pyrrolidine amide derivatives asMedChemComm · 2019Article
- Molecular mechanism of activation of the immunoregulatory amidase NAAA.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- Secretion, isotopic labeling and deglycosylation of N-acylethanolamine acid amidase for biophysical studies.Protein expression and purification · 2018Article
- Dysfunctional oleoylethanolamide signaling in a mouse model of Prader-Willi syndrome.Pharmacological research · 2017Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
19 authors at 3 institutions in 2 countries.
Funding
Abstract
Palmitoylethanolamide (PEA) and oleoylethanolamide (OEA) are endogenous lipid mediators that suppress inflammation. Their actions are terminated by the intracellular cysteine amidase, N-acylethanolamine acid amidase (NAAA). Even though NAAA may offer a new target for anti-inflammatory therapy, the lipid-like structures and reactive warheads of current NAAA inhibitors limit the use of these agents as oral drugs. A series of novel benzothiazole-piperazine derivatives that inhibit NAAA in a potent and selective manner by a non-covalent mechanism are described. A prototype member of this class (8) displays high oral bioavailability, access to the central nervous system (CNS), and strong activity in a mouse model of multiple sclerosis (MS). This compound exemplifies a second generation of non-covalent NAAA inhibitors that may be useful in the treatment of MS and other chronic CNS disorders.
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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.