Synthesis, activity and mechanism of alkoxy-, carbamato-, sulfonamido-, thioureido-, and ureido-derivatives of 2,4,5-trimethylpyridin-3-ol against inflammatory bowel disease
DC Field | Value | Language |
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dc.contributor.author | Chaudhary, Chhabi Lal | - |
dc.contributor.author | Gurung, Pallavi | - |
dc.contributor.author | Jang, Seoul | - |
dc.contributor.author | Banskota, Suhrid | - |
dc.contributor.author | Nam, Tae-Gyu | - |
dc.contributor.author | Kim, Jung-Ae | - |
dc.contributor.author | Jeong, Byeong-Seon | - |
dc.date.accessioned | 2021-06-22T09:08:42Z | - |
dc.date.available | 2021-06-22T09:08:42Z | - |
dc.date.created | 2021-01-21 | - |
dc.date.issued | 2020-01 | - |
dc.identifier.issn | 1475-6366 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/1370 | - |
dc.description.abstract | Inflammatory bowel disease (IBD) is a chronic immuno-inflammation in gastrointestinal tract. We have evaluated the activity of the compounds to inhibit the adhesion of monocytes to colon epithelial cells is triggered by a pro-inflammatory cytokine, tumour necrosis factor (TNF)-?. The in vitro activity of the compounds, 13b (an ureido-derivative), 14c, 14j, 14k, 14n (thioureido-), 18c and 18d (sulfonamido-), was in correlation with in vivo anti-colitis activity revealed as significant recovery in body- and colon-weights and colon myeloperoxidase level, a biochemical marker of inflammation reflecting neutrophil infiltration. In vivo, TNBS-induced changes in the expression of inflammatory cytokines (TNF-?, IL-6, IL-1?, IL-10, and TGF-?), NLRP3 inflammasome components (NLRP-3, Caspase-1, and IL-18), and epithelial junction molecules (E-cadherin, claudin2/3, and ZO-1) were blocked and recovered by oral administration of the compounds (1?mg/kg). Compound 14n which showed the best efficacy can be a promising lead for orally available therapeutics for pathology of IBD. | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | TAYLOR & FRANCIS LTD | - |
dc.title | Synthesis, activity and mechanism of alkoxy-, carbamato-, sulfonamido-, thioureido-, and ureido-derivatives of 2,4,5-trimethylpyridin-3-ol against inflammatory bowel disease | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Nam, Tae-Gyu | - |
dc.identifier.doi | 10.1080/14756366.2019.1677637 | - |
dc.identifier.scopusid | 2-s2.0-85073461381 | - |
dc.identifier.wosid | 000490609000001 | - |
dc.identifier.bibliographicCitation | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, v.35, no.1, pp.1 - 20 | - |
dc.relation.isPartOf | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | - |
dc.citation.title | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | - |
dc.citation.volume | 35 | - |
dc.citation.number | 1 | - |
dc.citation.startPage | 1 | - |
dc.citation.endPage | 20 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.isOpenAccess | N | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Biochemistry & Molecular Biology | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Biochemistry & Molecular Biology | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.subject.keywordPlus | TGF-BETA | - |
dc.subject.keywordPlus | INDUCED COLITIS | - |
dc.subject.keywordPlus | EXPRESSION | - |
dc.subject.keywordPlus | IL-10 | - |
dc.subject.keywordPlus | ALPHA | - |
dc.subject.keywordPlus | IMMUNITY | - |
dc.subject.keywordPlus | INNATE | - |
dc.subject.keywordPlus | CELLS | - |
dc.subject.keywordPlus | 6-AMINO-2,4,5-TRIMETHYLPYRIDIN-3-OLS | - |
dc.subject.keywordPlus | CLOTRIMAZOLE | - |
dc.subject.keywordAuthor | Pyridin-3-ols | - |
dc.subject.keywordAuthor | inflammatory bowel disease | - |
dc.subject.keywordAuthor | TNF-? | - |
dc.subject.keywordAuthor | adhesion | - |
dc.subject.keywordAuthor | epithelial junction | - |
dc.identifier.url | https://www.tandfonline.com/doi/full/10.1080/14756366.2019.1677637 | - |
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