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Synthesis, Characterization, and in vitro Anti-Inflammatory Activity of Novel Ferrocenyl(Piperazine-1-Yl)Methanone-based Derivatives

文献类型： 外文期刊

作者： Ruan, Banfeng 1 ; Li, Jin 1 ; Guo, Qinglei 1 ; Zhang, Min 1 ; Pei, Zhouyang 2 ; Hu, Yong 3 ;

作者机构： 1.Hefei Univ, Sch Biol Food & Environm, Hefei 230601, Peoples R China

2.Anhui Wannan Tobacco Co Ltd, Xuancheng 242000, Peoples R China

3.Anhui Acad Agr Sci, Agroprod Proc Res Inst, Hefei 230001, Peoples R China

关键词： Ferrocene; sulfamides; carboxamides; synthesis; anti-inflammatory activity; macrophages

期刊名称：MEDICINAL CHEMISTRY （ 影响因子：2.3； 五年影响因子：2.3 ）

ISSN： 1573-4064

年卷期： 2023 年 19 卷 9 期

页码：

收录情况： SCI

摘要： Background: Inflammation is closely related to the occurrence and development of various diseases in the clinical scope. Finding effective anti-inflammatory agents is of great significance for clinical treatment. A series of novel ferrocenyl(piperazine-1-yl)methanone-based sulfamides and carboxamides were synthesized to discover potent anti-inflammatory agents. Methods: The compounds were characterized by H-1 NMR, C-13 NMR, and MS spectra. Compound 5h was further determined by single crystal X-ray diffraction. All the target compounds were screened for anti-inflammatory activity by evaluating the inhibition effect of LPS-induced NO production in RAW264.7 macrophages. The novel compound (4i) is the preliminary anti-inflammatory mechanism detected by western blot. Results: In a multi-stage screening campaign, compound 4i was shortlisted, which exhibited physicochemical properties suitable for human administration. Among them, compound 4i was found to be most potent in inhibiting NO production (IC50 = 7.65 mu M) with low toxicity. This compound also exhibited significant inhibition of the production of iNOS and COX-2. Preliminary mechanism studies indicated that compound 4i could inhibit the activation of the LPS-induced TLR4/NF-kappa B signaling pathway. Conclusion: The promising anti-inflammatory activity of compound 4i compared with the reference drug suggests that this compound may contribute as a lead compound in the search for new potential anti-inflammatory agents.

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