Synthesis and anti-rheumatoid arthritis activities of 3-(4-aminophenyl)-coumarin derivatives
| Autor: | Jie Sun, Yuhang Miao, Jie Yang, Yinling Yun, Wang Xiaojing |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
rheumatoid arthritis
Systemic disease Unknown aetiology Anti-Inflammatory Agents RM1-950 01 natural sciences Arthritis Rheumatoid Rats Sprague-Dawley chemistry.chemical_compound Structure-Activity Relationship Coumarins Synovitis Drug Discovery Medicine Animals Humans Cells Cultured Cell Proliferation Pharmacology 3-(4-Aminophenyl)-coumarin Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry business.industry Anti inflammation General Medicine medicine.disease Coumarin anti-inflammation 0104 chemical sciences Rats 010404 medicinal & biomolecular chemistry Disease Models Animal chemistry RA-FLSs proliferation inhibition Dysplasia Rheumatoid arthritis Immunology Cytokines Therapeutics. Pharmacology business Research Article Research Paper |
| Zdroj: | Journal of Enzyme Inhibition and Medicinal Chemistry article-version (VoR) Version of Record Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 36, Iss 1, Pp 450-461 (2021) |
| ISSN: | 1475-6374 |
| Popis: | Rheumatoid arthritis is a chronic systemic disease characterised by an unknown aetiology of inflammatory synovitis. A large number of studies have shown that synoviocytes show tumour-like dysplasia in the pathological process of RA, and the changes in the expression of related cytokines are closely related to the pathogenesis of RA. In this thesis, a series of novel 3-(4-aminophenyl) coumarins containing different substituents were synthesised to find new coumarin anti-inflammatory drugs for the treatment of rheumatoid arthritis. The results of preliminary activity screening showed that compound 5e had the strongest inhibitory activity on the proliferation of fibroid synovial cells, and it also had inhibitory effect on RA-related cytokines IL-1, IL-6, and TNF-α. The preliminary mechanism study showed that compound 5e could inhibit the activation of NF-κB and MAPKs signal pathway. The anti-inflammatory activity of compound 5e in vivo was further determined in the rat joint inflammation model. |
| Databáze: | OpenAIRE |
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