ArticleJournal of medicinal chemistry2014
CB2-selective cannabinoid receptor ligands: synthesis, pharmacological evaluation, and molecular modeling investigation of 1,8-Naphthyridin-2(1H)-one-3-carboxamides.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
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Who cites it
22 citing papers in PubMed.
- Transient receptor potential vanilloid 2 functions as a directional driver for hepoxilin AScience advances · 2026Article
- Synthesis of 2‑Quinolones via Thiolate-Mediated Cyclization of (ACS omega · 2026Article
- Development of Carborane-Based Halogenated Naphthyridinone-Analogues as Cannabinoid Receptor Type 2 (CBChemMedChem · 2025Article
- Development of Carborane-Based Benzothiazole Analogues as Cannabinoid Receptor Type 2 (CBACS omega · 2025Article
- Discovery of Potent and Selective CB2 Agonists Utilizing a Function-Based Computational Screening Protocol.ACS chemical neuroscience · 2023Article
- Synthesis, Structure-Activity Relationships, Radiofluorination, and Biological Evaluation of [Journal of medicinal chemistry · 2023Article
- Development of the High-Affinity Carborane-Based Cannabinoid Receptor Type 2 PET Ligand [Journal of medicinal chemistry · 2023Article
- Novel Cannabinoid Receptor 2 (CB2) Low Lipophilicity Agonists Produce Distinct cAMP and Arrestin Signalling Kinetics without Bias.International journal of molecular sciences · 2023Article
- New Insights into Bitopic Orthosteric/Allosteric Ligands of Cannabinoid Receptor Type 2.International journal of molecular sciences · 2023Article
- Rational drug design of CB2 receptor ligands: from 2012 to 2021.RSC advances · 2022Review
- Synthesis and In Vitro Characterization of Selective Cannabinoid CB2 Receptor Agonists: Biological Evaluation against Neuroblastoma Cancer Cells.Molecules (Basel, Switzerland) · 2022Article
- Design, synthesis and biological evaluation of novel orthosteric-allosteric ligands of the cannabinoid receptor type 2 (CBFrontiers in chemistry · 2022Article
- Molecular Targets of Cannabinoids Associated with Depression.Current medicinal chemistry · 2022Review
- Anti-Inflammatory Activity of a CB2 Selective Cannabinoid Receptor Agonist: Signaling and Cytokines Release in Blood Mononuclear Cells.Molecules (Basel, Switzerland) · 2021Article
- Development of [International journal of molecular sciences · 2021Article
- Development of selective, fluorescent cannabinoid type 2 receptor ligands based on a 1,8-naphthyridin-2-(1MedChemComm · 2018Article
- Synthesis and biological evaluation of 3-(1,3,4-oxadiazol-2-yl)-1,8-naphthyridin-4(1MedChemComm · 2018Article
- Anti-Proliferative Properties and Proapoptotic Function of New CB2 Selective Cannabinoid Receptor Agonist in Jurkat Leukemia Cells.International journal of molecular sciences · 2018Article
- Structure-Activity Relationship of Cannabis Derived Compounds for the Treatment of Neuronal Activity-Related Diseases.Molecules (Basel, Switzerland) · 2018Review
- Selective Cannabinoid 2 Receptor Stimulation Reduces Tubular Epithelial Cell Damage after Renal Ischemia-Reperfusion Injury.The Journal of pharmacology and experimental therapeutics · 2018Article
Corrections and comments
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Authors and funding
16 authors.
Funding
Abstract
We have recently identified 1,8-naphthyridin-2(1H)-one-3-carboxamide as a new scaffold very suitable for the development of new CB2 receptor potent and selective ligands. In this paper we describe a number of additional derivatives in which the same central scaffold has been variously functionalized in position 1 or 6. All new compounds showed high selectivity and affinity in the nanomolar range for the CB2 receptor. Furthermore, we found that their functional activity is controlled by the presence of the substituents at position C-6 of the naphthyridine scaffold. In fact, the introduction of substituents in this position determined a functionality switch from agonist to antagonists/inverse agonists. Finally, docking studies showed that the difference between the pharmacology of these ligands may be in the ability/inability to block the Toggle Switch W6.48(258) (χ1 g+ → trans) transition.
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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.