دورية أكاديمية
Design, synthesis and anti-inflammatory activity of imidazol-5-yl pyridine derivatives as p38α/MAPK14 inhibitor.
| العنوان: | Design, synthesis and anti-inflammatory activity of imidazol-5-yl pyridine derivatives as p38α/MAPK14 inhibitor. |
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| المؤلفون: | Ali EMH; Center for Biomaterials, Korea Institute of Science & Technology (KIST School), Seoul, Seongbuk-gu, 02792, Republic of Korea; University of Science & Technology (UST), Daejeon, Yuseong-gu, 34113, Republic of Korea; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Modern University for Technology and Information (MTI), Cairo 12055, Egypt., Abdel-Maksoud MS; Medicinal & Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre (NRC), (ID: 60014618), P.O. 12622, Dokki, Giza, Egypt., Hassan RM; Medicinal & Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre (NRC), (ID: 60014618), P.O. 12622, Dokki, Giza, Egypt., Mersal KI; Center for Biomaterials, Korea Institute of Science & Technology (KIST School), Seoul, Seongbuk-gu, 02792, Republic of Korea; University of Science & Technology (UST), Daejeon, Yuseong-gu, 34113, Republic of Korea., Ammar UM; Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, 161 Cathedral Street, Glasgow G4 0NR, Scotland, United Kingdom., Se-In C; Department of Pharmaceutical Biochemistry, College of Pharmacy, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Republic of Korea., He-Soo H; Department of Pharmaceutical Biochemistry, College of Pharmacy, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Republic of Korea., Kim HK; Department of Nuclear Medicine, Molecular Imaging & Therapeutic Medicine Research Center, Jeonbuk National University Medical School and Hospital, 20 Geonji-ro, Deokjin-gu, Jeonju 54907, Republic of Korea; Research Institute of Clinical Medicine of Jeonbuk National University-Biomedical Research Institute of Jeonbuk National University Hospital, 20 Geonji-ro, Deokjin-gu, Jeonju 54907, Republic of Korea., Lee A; Department of Chemistry, Hanseo University, Seosan 31962, Republic of Korea., Lee KT; Department of Pharmaceutical Biochemistry, College of Pharmacy, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Republic of Korea. Electronic address: ktlee@khu.ac.kr., Oh CH; Center for Biomaterials, Korea Institute of Science & Technology (KIST School), Seoul, Seongbuk-gu, 02792, Republic of Korea; University of Science & Technology (UST), Daejeon, Yuseong-gu, 34113, Republic of Korea. Electronic address: choh@kist.re.kr. |
| المصدر: | Bioorganic & medicinal chemistry [Bioorg Med Chem] 2021 Feb 01; Vol. 31, pp. 115969. Date of Electronic Publication: 2020 Dec 28. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Country of Publication: England NLM ID: 9413298 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3391 (Electronic) Linking ISSN: 09680896 NLM ISO Abbreviation: Bioorg Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Original Publication: Oxford : New York : Pergamon Press, c1993- |
| مواضيع طبية MeSH: | Drug Design*, Anti-Inflammatory Agents, Non-Steroidal/*pharmacology , Imidazoles/*pharmacology , Protein Kinase Inhibitors/*pharmacology , Pyridines/*pharmacology, Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis ; Anti-Inflammatory Agents, Non-Steroidal/chemistry ; Dose-Response Relationship, Drug ; Humans ; Imidazoles/chemical synthesis ; Imidazoles/chemistry ; Mitogen-Activated Protein Kinase 14/antagonists & inhibitors ; Mitogen-Activated Protein Kinase 14/metabolism ; Molecular Structure ; Protein Kinase Inhibitors/chemical synthesis ; Protein Kinase Inhibitors/chemistry ; Pyridines/chemical synthesis ; Pyridines/chemistry ; Structure-Activity Relationship ; THP-1 Cells ; p38 Mitogen-Activated Protein Kinases/antagonists & inhibitors ; p38 Mitogen-Activated Protein Kinases/metabolism |
| مستخلص: | P38α/MAPK14 is intracellular signalling regulator involved in biosynthesis of inflammatory mediator cytokines (TNF-α, IL-1, IL-6, and IL-1b), which induce the production of inflammatory proteins (iNOS, NF-kB, and COX-2). In this study, drug repurposing strategies were followed to repositioning of a series of B-RAF V600E imidazol-5-yl pyridine inhibitors to inhibit P38α kinase. A group 25 reported P38α kinase inhibitors were used to build a pharmacophore model for mapping the target compounds and proving their affinity for binding in P38α active site. Target compounds were evaluated for their potency against P38α kinase, compounds 11a and 11d were the most potent inhibitors (IC (Copyright © 2020 Elsevier Ltd. All rights reserved.) |
| فهرسة مساهمة: | Keywords: 1L-1β Nitric Oxide; 1L-6; Anti- inflammatory; P38α; PGE2; Pharmacophore; TNF-α |
| المشرفين على المادة: | 0 (Anti-Inflammatory Agents, Non-Steroidal) 0 (Imidazoles) 0 (Protein Kinase Inhibitors) 0 (Pyridines) 7GBN705NH1 (imidazole) EC 2.7.11.24 (Mitogen-Activated Protein Kinase 14) EC 2.7.11.24 (p38 Mitogen-Activated Protein Kinases) NH9L3PP67S (pyridine) |
| تواريخ الأحداث: | Date Created: 20210110 Date Completed: 20210831 Latest Revision: 20210831 |
| رمز التحديث: | 20240829 |
| DOI: | 10.1016/j.bmc.2020.115969 |
| PMID: | 33422910 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1464-3391 |
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| DOI: | 10.1016/j.bmc.2020.115969 |