Synthesis and in vitro and in vivo anti-inflammatory activity of novel 4-ferrocenylchroman-2-one derivatives

Autor: Wei-Yun Guo, Liu-Zeng Chen, Bang-Nian Shen, Xin-Hua Liu, Guang-Ping Tai, Qing-Shan Li, Li Gao, Ban-Feng Ruan
Jazyk: angličtina
Rok vydání: 2019
Předmět:
Zdroj: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 1678-1689 (2019)
Druh dokumentu: article
ISSN: 1475-6366
1475-6374
14756366
DOI: 10.1080/14756366.2019.1664499
Popis: A series of novel 4-ferrocenylchroman-2-one derivatives were designed and synthesised to discover potent anti-inflammatory agents for treatment of arthritis. All the target compounds had been screened for their anti-inflammatory activity by evaluating the inhibition effect of LPS-induced NO production in RAW 264.7 macrophages. Among them, 4-ferrocenyl-3,4-dihydro-2H-benzo[g]chromen-2-one (3h) was found to be the most potent compound in inhibiting the productions of NO with low toxicity. This compound also exhibited significant inhibition of the productions of IL-6 and TNF-α in RAW 264.7 macrophages. Preliminary mechanism studies indicated that compound 3h could inhibit the activation of LPS-induced NF-κB and MAPKs signalling pathways. The in vivo anti-inflammatory effect of this compound was determined in the rat adjuvant-induced arthritis model.
Databáze: Directory of Open Access Journals
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