ArticleEuropean journal of medicinal chemistry2022
Development of sulfonamide-based NLRP3 inhibitors: Further modifications and optimization through structure-activity relationship studies.
Article in European journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed.
- Exploring molecular frameworks for modulating NLRP3-driven neuroinflammation in Alzheimer's disease.Molecular diversity · 2026Review
- Discovery of a brain penetrant NLRP3 inflammasome inhibitor that reduces neuropathic pain in mice.European journal of medicinal chemistry · 2026Article
- Structural and functional evolution of IL-1 targeting: From systemic neutralization to bioengineered nanotherapies.Materials today. Bio · 2026Review
- Mechanistic Characterization of a Small Molecule as a Direct NLRP3 Inhibitor via Binding to the NACHT Domain.Journal of medicinal chemistry · 2025Article
- The NLRP3-P2X7 Axis and Cytokine Crosstalk in Alzheimer's Disease: Mechanisms, Implications, and Therapeutic Opportunities.CNS & neurological disorders drug targets · 2025Review
- NLRP3 inflammasome in cardiovascular diseases: an update.Frontiers in immunology · 2025Review
- Biological and therapeutic significance of targeting NLRP3 inflammasome in the brain and the current efforts to develop brain-penetrant inhibitors.Advances in pharmacology (San Diego, Calif.) · 2025Review
- Functional Characterization of an Arylsulfonamide-Based Small-Molecule Inhibitor of the NLRP3 Inflammasome.ACS chemical neuroscience · 2024Article
- Characterization of a small molecule inhibitor of the NLRP3 inflammasome and its potential use for acute lung injury.Bioorganic chemistry · 2024Article
- Role of NLRP3 in Parkinson's disease: Specific activation especially in dopaminergic neurons.Heliyon · 2024Review
- Design and Discovery of Novel NLRP3 Inhibitors and PET Imaging Radiotracers Based on a 1,2,3-Triazole-Bearing Scaffold.Journal of medicinal chemistry · 2024Article
- Targeting NLRP3 Inflammasome: Structure, Function, and Inhibitors.Current medicinal chemistry · 2024Article
- Drugging the NLRP3 inflammasome: from signalling mechanisms to therapeutic targets.Nature reviews. Drug discovery · 2024Review
- Chalcone: A potential scaffold for NLRP3 inflammasome inhibitors.European journal of medicinal chemistry reports · 2023Article
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8 authors.
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Abstract
NLRP3 inflammasome dysregulation has been observed in many human diseases including neurodegenerative disorders. Thus, development of small molecule inhibitors targeting this protein complex represents a promising strategy to achieve disease intervention. In our continuing efforts to develop NLRP3 inhibitors, a recently identified lead inhibitor, YQ128, was further modified and optimized. The structure-activity relationship studies of this lead compound suggested its flexibility for structural modifications while the sulfonamide and benzyl moiety demonstrated being important for selectivity. Additionally, the systematic SAR studies also provided insights for designing NLRC4 and AIM2 inflammasome inhibitors. A new lead inhibitor, 19, was identified with improved potency (IC
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