Synthesis and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-alpha-induced cell adhesion and inflammatory bowel disease
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Park, Sang Won | - |
dc.contributor.author | Banskota, Suhrid | - |
dc.contributor.author | Gurung, Pallavi | - |
dc.contributor.author | Jin, You Jin | - |
dc.contributor.author | Kang, Han-eol | - |
dc.contributor.author | Chaudhary, Chhabi Lat | - |
dc.contributor.author | Lee, Sang Yeul | - |
dc.contributor.author | Jeong, Byeong-Seon | - |
dc.contributor.author | Kim, Jung-Ae | - |
dc.contributor.author | Nam, Tae-gyu | - |
dc.date.accessioned | 2021-06-22T11:41:58Z | - |
dc.date.available | 2021-06-22T11:41:58Z | - |
dc.date.created | 2021-01-21 | - |
dc.date.issued | 2018-08 | - |
dc.identifier.issn | 2040-2503 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/5710 | - |
dc.description.abstract | Inflammatory bowel disease (IBD) is an inflammatory disease of the gastrointestinal tract with complex pathogenesis. Here, we synthesized 6-heteroarylamino analogues to inhibit TNF-alpha-induced adhesion of monocytes to colon epithelial cells which are implicated in the initial inflammation process of IBD. The best analogue, 16a, showed IC50 = 0.29 mu M, which is about five orders of magnitude better than that of 5-aminosalicylic acid (5-ASA), a positive control. Oral administration of 6f and 16a dramatically ameliorated 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced colon inflammation in rat. The ameliorating effects were accompanied by a high level of recovery in colon and body weights and in the myeloperoxidase (MPO) level. Consistently, the compounds suppressed the expression of intercellular adhesion molecule-1 (ICAM-1) and monocyte chemoattractant protein 1 (MCP-1). Moreover, they significantly suppressed the expression of pro-inflammatory cytokines such as TNF-alpha, IL-1 beta, and IL-6 while increasing the level of IL-10, an anti-inflammatory cytokine. | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | ROYAL SOC CHEMISTRY | - |
dc.title | Synthesis and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-alpha-induced cell adhesion and inflammatory bowel disease | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Nam, Tae-gyu | - |
dc.identifier.doi | 10.1039/c8md00156a | - |
dc.identifier.scopusid | 2-s2.0-85051657477 | - |
dc.identifier.wosid | 000442751800006 | - |
dc.identifier.bibliographicCitation | MEDCHEMCOMM, v.9, no.8, pp.1305 - 1310 | - |
dc.relation.isPartOf | MEDCHEMCOMM | - |
dc.citation.title | MEDCHEMCOMM | - |
dc.citation.volume | 9 | - |
dc.citation.number | 8 | - |
dc.citation.startPage | 1305 | - |
dc.citation.endPage | 1310 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.isOpenAccess | Y | - |
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 | INTESTINAL INFLAMMATION | - |
dc.subject.keywordPlus | THERAPEUTIC TARGETS | - |
dc.subject.keywordPlus | CROHNS-DISEASE | - |
dc.subject.keywordPlus | IBD | - |
dc.subject.keywordPlus | PATHOGENESIS | - |
dc.subject.keywordPlus | 6-AMINO-2,4,5-TRIMETHYLPYRIDIN-3-OLS | - |
dc.subject.keywordPlus | IL-10 | - |
dc.subject.keywordPlus | ASSAY | - |
dc.subject.keywordPlus | RAT | - |
dc.subject.keywordAuthor | INTESTINAL INFLAMMATION | - |
dc.subject.keywordAuthor | THERAPEUTIC TARGETS | - |
dc.subject.keywordAuthor | CROHNS-DISEASE | - |
dc.subject.keywordAuthor | IBD | - |
dc.subject.keywordAuthor | PATHOGENESIS6-AMINO-2,4,5-TRIMETHYLPYRIDIN-3-OLS | - |
dc.subject.keywordAuthor | IL-10 | - |
dc.subject.keywordAuthor | ASSAY | - |
dc.subject.keywordAuthor | RAT | - |
dc.identifier.url | https://pubs.rsc.org/en/content/articlelanding/2018/MD/C8MD00156A | - |
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.
55 Hanyangdeahak-ro, Sangnok-gu, Ansan, Gyeonggi-do, 15588, Korea+82-31-400-4269 sweetbrain@hanyang.ac.kr
COPYRIGHT © 2021 HANYANG UNIVERSITY. ALL RIGHTS RESERVED.
Certain data included herein are derived from the © Web of Science of Clarivate Analytics. All rights reserved.
You may not copy or re-distribute this material in whole or in part without the prior written consent of Clarivate Analytics.