دورية أكاديمية
Anti-inflammatory effect of 3-fluorophenyl pyrimidinylimidazo[2,1-b]thiazole derivatives as p38α inhibitors.
| العنوان: | Anti-inflammatory effect of 3-fluorophenyl pyrimidinylimidazo[2,1-b]thiazole derivatives as p38α inhibitors. |
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| المؤلفون: | Al-Sanea MM; Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka 72341, Saudi Arabia. Electronic address: ms.abdel-maksoud@nrc.sci.eg., Abdel-Maksoud MS; Medicinal and Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Institute, National Research Centre (ID: 60014618), Dokki, Giza, Egypt. Electronic address: ph_ss@hotmail.com., El-Behairy MF; Department of Organic and Medicinal Chemistry, Faculty of Pharmacy, University of Sadat City, Menoufiya 32897, Egypt., Hamdi A; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt., Ur Rahman H; Department of Clinical Pharmacy, College of Pharmacy, Jouf University, Sakaka, Aljouf 72341, Saudi Arabia., Parambi DGT; Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka 72341, Saudi Arabia., Elbargisy RM; Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Al-Jouf, Saudi Arabia., Mohamed AAB; Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt. |
| المصدر: | Bioorganic chemistry [Bioorg Chem] 2023 Oct; Vol. 139, pp. 106716. Date of Electronic Publication: 2023 Jul 13. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Country of Publication: United States NLM ID: 1303703 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1090-2120 (Electronic) Linking ISSN: 00452068 NLM ISO Abbreviation: Bioorg Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Amsterdam : Elsevier Original Publication: New York, London, Academic Press. |
| مواضيع طبية MeSH: | Thiazoles*/pharmacology , Nitric Oxide*, Molecular Docking Simulation ; Anti-Inflammatory Agents/pharmacology ; Anti-Inflammatory Agents/chemistry ; Sulfonamides/chemistry ; Amides ; Pyrimidines/pharmacology ; Structure-Activity Relationship ; Molecular Structure |
| مستخلص: | In the present work, the anti-inflammatory effect of 30 compounds containing 3-fluorophenyl pyrimidinylimidazo[2,1-b]thiazole was investigated. All final target compounds showed significant Inhibitory effect on p38α. P38α is considered one of the key kinases in the inflammatory process due to its regulatory effect on pro-inflammatory mediators. The final target compounds divided into four group based on the type of terminal moiety (amide and sulfonamide) and the linker between pyrimidine ring and terminal moiety (ethyl and propyl). Most compounds with terminal sulfonamide moiety and propyl linker between the sulfonamide and pyrimidine ring were the most potent among all synthesized final target compounds with sub-micromolar IC Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. (Copyright © 2023 Elsevier Inc. All rights reserved.) |
| فهرسة مساهمة: | Keywords: Amide; Antiinflammatory; P38α inhibitors; Sulfonamide, pyrimidinylimidazo[2,1-b]thiazole |
| المشرفين على المادة: | 0 (Thiazoles) 31C4KY9ESH (Nitric Oxide) 0 (Anti-Inflammatory Agents) 0 (Sulfonamides) 0 (Amides) 0 (Pyrimidines) |
| تواريخ الأحداث: | Date Created: 20230717 Date Completed: 20230814 Latest Revision: 20230814 |
| رمز التحديث: | 20231215 |
| DOI: | 10.1016/j.bioorg.2023.106716 |
| PMID: | 37459825 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1090-2120 |
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| DOI: | 10.1016/j.bioorg.2023.106716 |