{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,11,14]],"date-time":"2026-11-14T04:48:52Z","timestamp":1794631732815,"version":"4.9.1"},"reference-count":35,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2025,11,1]],"date-time":"2025-11-01T00:00:00Z","timestamp":1761955200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2025,11,1]],"date-time":"2025-11-01T00:00:00Z","timestamp":1761955200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2025,11,1]],"date-time":"2025-11-01T00:00:00Z","timestamp":1761955200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2025,11,1]],"date-time":"2025-11-01T00:00:00Z","timestamp":1761955200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2025,11,1]],"date-time":"2025-11-01T00:00:00Z","timestamp":1761955200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2025,11,1]],"date-time":"2025-11-01T00:00:00Z","timestamp":1761955200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2025,11,1]],"date-time":"2025-11-01T00:00:00Z","timestamp":1761955200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81803364"],"award-info":[{"award-number":["81803364"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81872743"],"award-info":[{"award-number":["81872743"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["European Journal of Medicinal Chemistry"],"published-print":{"date-parts":[[2025,11]]},"DOI":"10.1016\/j.ejmech.2025.118023","type":"journal-article","created":{"date-parts":[[2025,8,5]],"date-time":"2025-08-05T21:11:47Z","timestamp":1754428307000},"page":"118023","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":4,"special_numbering":"C","title":["Discovery of novel 8-hydroxyquinoline derivatives as NLRP3 inflammasome inhibitors with therapeutic potential for inflammatory bowel disease"],"prefix":"10.1016","volume":"298","author":[{"given":"Xiuxiu","family":"Zhang","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ruiwen","family":"Wu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yuyun","family":"Yan","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yiming","family":"Luo","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zhipeng","family":"Wan","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zhuorong","family":"Liu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xiangting","family":"Liang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jie","family":"Yang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dan","family":"Wu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ping","family":"Sun","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wenhui","family":"Hu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1235-0804","authenticated-orcid":false,"given":"Zhongjin","family":"Yang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.ejmech.2025.118023_bib1","doi-asserted-by":"crossref","first-page":"331","DOI":"10.1016\/j.tibs.2022.10.002","article-title":"The NLRP3 inflammasome: activation and regulation","volume":"48","author":"Xu","year":"2023","journal-title":"Trends Biochem. Sci."},{"key":"10.1016\/j.ejmech.2025.118023_bib2","doi-asserted-by":"crossref","first-page":"2288","DOI":"10.1016\/j.cell.2023.04.025","article-title":"A 360\u00b0 view of the inflammasome: mechanisms of activation, cell death, and diseases","volume":"186","author":"Barnett","year":"2023","journal-title":"Cell"},{"key":"10.1016\/j.ejmech.2025.118023_bib3","doi-asserted-by":"crossref","first-page":"477","DOI":"10.1038\/s41577-019-0165-0","article-title":"The NLRP3 inflammasome: molecular activation and regulation to therapeutics","volume":"19","author":"Swanson","year":"2019","journal-title":"Nat. Rev. Immunol."},{"key":"10.1016\/j.ejmech.2025.118023_bib4","doi-asserted-by":"crossref","first-page":"338","DOI":"10.1038\/s41586-019-1295-z","article-title":"Structural mechanism for NEK7-licensed activation of NLRP3 inflammasome","volume":"570","author":"Sharif","year":"2019","journal-title":"Nature"},{"key":"10.1016\/j.ejmech.2025.118023_bib5","doi-asserted-by":"crossref","first-page":"128","DOI":"10.1038\/s41419-019-1413-8","article-title":"Recent advances in the mechanisms of NLRP3 inflammasome activation and its inhibitors","volume":"10","author":"Yang","year":"2019","journal-title":"Cell Death Dis."},{"key":"10.1016\/j.ejmech.2025.118023_bib6","doi-asserted-by":"crossref","first-page":"321","DOI":"10.1146\/annurev-immunol-030409-101311","article-title":"The Sterile inflammatory response","volume":"28","author":"Rock","year":"2010","journal-title":"Annu. Rev. Immunol."},{"key":"10.1016\/j.ejmech.2025.118023_bib7","doi-asserted-by":"crossref","first-page":"588","DOI":"10.1038\/nrd.2018.97","article-title":"Targeting the NLRP3 inflammasome in inflammatory diseases","volume":"17","author":"Mangan","year":"2018","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2025.118023_bib8","doi-asserted-by":"crossref","first-page":"189","DOI":"10.1016\/j.cytogfr.2011.10.001","article-title":"Understanding the mechanism of IL-1\u03b2 secretion","volume":"22","author":"Lopez-Castejon","year":"2011","journal-title":"Cytokine Growth Factor Rev."},{"key":"10.1016\/j.ejmech.2025.118023_bib9","doi-asserted-by":"crossref","first-page":"171","DOI":"10.1016\/j.it.2011.02.002","article-title":"The Nlrp3 inflammasome: contributions to intestinal homeostasis","volume":"32","author":"Zaki","year":"2011","journal-title":"Trends Immunol."},{"key":"10.1016\/j.ejmech.2025.118023_bib10","doi-asserted-by":"crossref","first-page":"639","DOI":"10.1038\/nrrheum.2017.155","article-title":"Inflammation in gout: mechanisms and therapeutic targets","volume":"13","author":"So","year":"2017","journal-title":"Nat. Rev. Rheumatol."},{"key":"10.1016\/j.ejmech.2025.118023_bib11","doi-asserted-by":"crossref","first-page":"194","DOI":"10.2337\/db12-0420","article-title":"Upregulated NLRP3 inflammasome activation in patients with type 2 diabetes","volume":"62","author":"Lee","year":"2013","journal-title":"Diabetes"},{"key":"10.1016\/j.ejmech.2025.118023_bib12","doi-asserted-by":"crossref","first-page":"127","DOI":"10.1016\/j.atherosclerosis.2017.10.027","article-title":"NLRP3 inflammasome pathways in atherosclerosis","volume":"267","author":"Baldrighi","year":"2017","journal-title":"Atherosclerosis"},{"key":"10.1016\/j.ejmech.2025.118023_bib13","doi-asserted-by":"crossref","first-page":"674","DOI":"10.1038\/nature11729","article-title":"NLRP3 is activated in Alzheimer's disease and contributes to pathology in APP\/PS1 mice","volume":"493","author":"Heneka","year":"2013","journal-title":"Nature"},{"key":"10.1016\/j.ejmech.2025.118023_bib14","doi-asserted-by":"crossref","first-page":"77","DOI":"10.1007\/s10787-017-0401-9","article-title":"Pharmacological inhibition of the NLRP3 inflammasome as a potential target for multiple sclerosis induced central neuropathic pain","volume":"26","author":"Khan","year":"2018","journal-title":"Inflammopharmacology"},{"key":"10.1016\/j.ejmech.2025.118023_bib15","doi-asserted-by":"crossref","first-page":"248","DOI":"10.1038\/nm.3806","article-title":"A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases","volume":"21","author":"Coll","year":"2015","journal-title":"Nat. Med."},{"key":"10.1016\/j.ejmech.2025.118023_bib16","series-title":"Preparation of Sulfonylureas and Related Compounds as Inhibitors of NLRP3 Inflammasome Activation for the Treatment of Diseases","author":"O'Neill","year":"2016"},{"key":"10.1016\/j.ejmech.2025.118023_bib17","doi-asserted-by":"crossref","DOI":"10.1002\/ctm2.1471","article-title":"A randomized, double-blind phase 1b study evaluating the safety, tolerability, pharmacokinetics and pharmacodynamics of the NLRP3 inhibitor selnoflast in patients with moderate to severe active ulcerative colitis","volume":"13","author":"Klughammer","year":"2023","journal-title":"Clin. Transl. Med."},{"key":"10.1016\/j.ejmech.2025.118023_bib18","doi-asserted-by":"crossref","DOI":"10.1111\/cts.13789","article-title":"First-in-human safety, tolerability, and pharmacokinetic results of DFV890, an oral low-molecular-weight NLRP3 inhibitor","volume":"17","author":"Gatlik","year":"2024","journal-title":"Clin Transl Sci"},{"key":"10.1016\/j.ejmech.2025.118023_bib19","doi-asserted-by":"crossref","first-page":"14721","DOI":"10.1021\/acs.jmedchem.2c01250","article-title":"Overcoming preclinical safety obstacles to discover (S)-N-((1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-3-sulfonamide (GDC-2394): a potent and selective NLRP3 inhibitor","volume":"65","author":"McBride","year":"2022","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.118023_bib20","doi-asserted-by":"crossref","first-page":"1438","DOI":"10.1021\/acsptsci.4c00061","volume":"7","author":"Doedens","year":"2024","journal-title":"ACS Pharmacol. Transl. Sci."},{"key":"10.1016\/j.ejmech.2025.118023_bib21","doi-asserted-by":"crossref","first-page":"202","DOI":"10.1002\/cpdd.1162","article-title":"Safety, tolerability, pharmacokinetics, and pharmacodynamics of the oral NLRP3 inflammasome inhibitor ZYIL1: first-in-human phase 1 studies (single ascending dose and multiple ascending dose)","volume":"12","author":"Parmar","year":"2023","journal-title":"Clin Pharmacol Drug Dev"},{"key":"10.1016\/j.ejmech.2025.118023_bib22","doi-asserted-by":"crossref","first-page":"14897","DOI":"10.1021\/acs.jmedchem.3c01398","article-title":"Discovery of clinical candidate NT-0796, a brain-penetrant and highly potent NLRP3 inflammasome inhibitor for neuroinflammatory disorders","volume":"66","author":"Harrison","year":"2023","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.118023_bib23","doi-asserted-by":"crossref","DOI":"10.1021\/acs.jmedchem.5c00781","article-title":"Discovery of AZD4144, a selective and potent NLRP3 inhibitor for the treatment of inflammatory diseases","author":"Johansson","year":"2025","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.118023_bib24","doi-asserted-by":"crossref","first-page":"20780","DOI":"10.1021\/acs.jmedchem.4c02350","article-title":"Discovery of NP3-253, a potent brain penetrant inhibitor of the NLRP3 inflammasome","volume":"67","author":"Mackay","year":"2024","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.118023_bib25","doi-asserted-by":"crossref","first-page":"e270","DOI":"10.1016\/S2665-9913(20)30065-5","article-title":"Dapansutrile, an oral selective NLRP3 inflammasome inhibitor, for treatment of gout flares: an open-label, dose-adaptive, proof-of-concept, phase 2a trial","volume":"2","author":"Kl\u00fcck","year":"2020","journal-title":"The Lancet Rheumatology"},{"key":"10.1016\/j.ejmech.2025.118023_bib26","doi-asserted-by":"crossref","first-page":"591","DOI":"10.1016\/j.bbrc.2005.01.159","article-title":"8-Hydroxyquinoline inhibits iNOS expression and nitric oxide production by down-regulating LPS-induced activity of NF-\u03baB and C\/EBP\u03b2 in raw 264.7 cells","volume":"329","author":"Kim","year":"2005","journal-title":"Biochem. Biophys. Res. Commun."},{"key":"10.1016\/j.ejmech.2025.118023_bib27","doi-asserted-by":"crossref","DOI":"10.1016\/j.cbi.2022.110122","article-title":"Chlorquinaldol inhibits the activation of nucleotide-binding oligomerization domain-like receptor family pyrin domain-containing protein 3 inflammasome and ameliorates imiquimod-induced psoriasis-like dermatitis in mice","volume":"365","author":"Chen","year":"2022","journal-title":"Chem. Biol. Interact."},{"key":"10.1016\/j.ejmech.2025.118023_bib28","doi-asserted-by":"crossref","first-page":"252","DOI":"10.1016\/j.ejmech.2016.05.007","article-title":"8-Hydroxyquinolines in medicinal chemistry: a structural perspective","volume":"120","author":"Oliveri","year":"2016","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.118023_bib29","doi-asserted-by":"crossref","first-page":"997","DOI":"10.1007\/s00210-020-02034-6","article-title":"Chloroquine\/hydroxychloroquine: an inflammasome inhibitor in severe COVID-19?","volume":"394","author":"Bahadoram","year":"2021","journal-title":"Naunyn-Schmiedebergs Arch Pharmacol"},{"key":"10.1016\/j.ejmech.2025.118023_bib30","doi-asserted-by":"crossref","first-page":"9181","DOI":"10.1002\/chem.201600926","article-title":"Synthetically tuning the 2-Position of halogenated quinolines: optimizing antibacterial and biofilm eradication activities via alkylation and reductive amination pathways","volume":"22","author":"Basak","year":"2016","journal-title":"Chemistry"},{"key":"10.1016\/j.ejmech.2025.118023_bib31","first-page":"1947","article-title":"Synthesis of novel 2-methyl-4-carboxyquinolines, the new by-products of the Doebner reaction","volume":"51","author":"Ghodsi","year":"2021","journal-title":"Synth. Commun."},{"key":"10.1016\/j.ejmech.2025.118023_bib32","doi-asserted-by":"crossref","first-page":"11639","DOI":"10.1021\/acs.jmedchem.0c00834","article-title":"Potent and selective human Prostaglandin F (FP) receptor antagonist (BAY-6672) for the treatment of idiopathic pulmonary fibrosis (IPF)","volume":"63","author":"Beck","year":"2020","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.118023_bib33","doi-asserted-by":"crossref","first-page":"9299","DOI":"10.1021\/ja010769r","article-title":"Metal cation complexation and activation of reversed CPyI analogues of CC-1065 and duocarmycin SA: partitioning the effects of binding and catalysis","volume":"123","author":"Ellis","year":"2001","journal-title":"J. Am. Chem. Soc."},{"key":"10.1016\/j.ejmech.2025.118023_bib34","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2021.113153","article-title":"Nitric oxide-donating and reactive oxygen species-responsive prochelators based on 8-hydroxyquinoline as anticancer agents","volume":"212","author":"Zhang","year":"2021","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.118023_bib35","doi-asserted-by":"crossref","first-page":"354","DOI":"10.1038\/nature16959","article-title":"NEK7 is an essential mediator of NLRP3 activation downstream of potassium efflux","volume":"530","author":"He","year":"2016","journal-title":"Nature"}],"container-title":["European Journal of Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523425007883?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523425007883?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2026,3,6]],"date-time":"2026-03-06T09:13:15Z","timestamp":1772788395000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0223523425007883"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2025,11]]},"references-count":35,"alternative-id":["S0223523425007883"],"URL":"https:\/\/doi.org\/10.1016\/j.ejmech.2025.118023","relation":{},"ISSN":["0223-5234"],"issn-type":[{"value":"0223-5234","type":"print"}],"subject":[],"published":{"date-parts":[[2025,11]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Discovery of novel 8-hydroxyquinoline derivatives as NLRP3 inflammasome inhibitors with therapeutic potential for inflammatory bowel disease","name":"articletitle","label":"Article Title"},{"value":"European Journal of Medicinal Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.ejmech.2025.118023","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2025 Elsevier Masson SAS. All rights are reserved, including those for text and data mining, AI training, and similar technologies.","name":"copyright","label":"Copyright"}],"article-number":"118023"}}