دورية أكاديمية
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Synthesis and biological evaluation of pyridine-linked indanone derivatives: Potential agents for inflammatory bowel disease.

التفاصيل البيبلوغرافية
العنوان: Synthesis and biological evaluation of pyridine-linked indanone derivatives: Potential agents for inflammatory bowel disease.
المؤلفون: Kadayat TM; College of Pharmacy, Yeungnam University, Gyeongsan 38541, Republic of Korea; New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu 41061, Republic of Korea., Banskota S; College of Pharmacy, Yeungnam University, Gyeongsan 38541, Republic of Korea., Bist G; College of Pharmacy, Yeungnam University, Gyeongsan 38541, Republic of Korea., Gurung P; College of Pharmacy, Yeungnam University, Gyeongsan 38541, Republic of Korea., Magar TBT; College of Pharmacy, Yeungnam University, Gyeongsan 38541, Republic of Korea., Shrestha A; College of Pharmacy, Yeungnam University, Gyeongsan 38541, Republic of Korea., Kim JA; College of Pharmacy, Yeungnam University, Gyeongsan 38541, Republic of Korea. Electronic address: jakim@yu.ac.kr., Lee ES; College of Pharmacy, Yeungnam University, Gyeongsan 38541, Republic of Korea. Electronic address: eslee@yu.ac.kr.
المصدر: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2018 Aug 01; Vol. 28 (14), pp. 2436-2441. Date of Electronic Publication: 2018 Jun 08.
نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE
أسماء مطبوعة: Publication: Oxford : Elsevier Science Ltd
Original Publication: Oxford ; New York : Pergamon Press, c1991-
مواضيع طبية MeSH: Anti-Inflammatory Agents, Non-Steroidal/*pharmacology , Indans/*pharmacology , Inflammatory Bowel Diseases/*drug therapy , Pyridines/*pharmacology, Administration, Oral ; Animals ; Anti-Inflammatory Agents, Non-Steroidal/administration & dosage ; Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis ; Cell Adhesion/drug effects ; Colitis/chemically induced ; Colitis/drug therapy ; Colitis/pathology ; Disease Models, Animal ; Dose-Response Relationship, Drug ; Epithelial Cells/drug effects ; Epithelial Cells/pathology ; HT29 Cells ; Humans ; Indans/administration & dosage ; Indans/chemical synthesis ; Inflammatory Bowel Diseases/pathology ; Molecular Structure ; Monocytes/drug effects ; Monocytes/metabolism ; Pyridines/administration & dosage ; Pyridines/chemistry ; Rats ; Structure-Activity Relationship ; Trinitrobenzenesulfonic Acid ; Tumor Necrosis Factor-alpha/metabolism
مستخلص: A series of pyridine-linked indanone derivatives were designed and synthesized to discover new small molecules for the treatment of inflammatory bowel disease (IBD). Compounds 5b and 5d exhibited strongest inhibitory activity against TNF-α-induced monocyte adhesion to colon epithelial cells (an in vitro model of colitis). In TNBS (2,4,6-trinitrobenzenesulfonic acid)-induced rat colitis model, oral administration of the compounds 5b and 5d ameliorated colitis with significant recovery in altered expressions of E-cadherin, TNF-α and IL-1β expressions, indicating 5b and 5d as potential agents for therapeutics development against IBD.
(Copyright © 2018 Elsevier Ltd. All rights reserved.)
فهرسة مساهمة: Keywords: Antiinflammatory agents; Inflammatory bowel disease; Pyridine-linked indanones; Synthesis; TNF-α
المشرفين على المادة: 0 (Anti-Inflammatory Agents, Non-Steroidal)
0 (Indans)
0 (Pyridines)
0 (Tumor Necrosis Factor-alpha)
8T3HQG2ZC4 (Trinitrobenzenesulfonic Acid)
NH9L3PP67S (pyridine)
تواريخ الأحداث: Date Created: 20180619 Date Completed: 20190213 Latest Revision: 20190215
رمز التحديث: 20221213
DOI: 10.1016/j.bmcl.2018.06.012
PMID: 29910080
قاعدة البيانات: MEDLINE
الوصف
تدمد:1464-3405
DOI:10.1016/j.bmcl.2018.06.012