β-氯代乙烯基查耳酮类化合物的合成及作为 TNF-α 和 IL-6 抑制剂的生物评价及其抗菌活性。
Synthesis and biological evaluation of beta-chloro vinyl chalcones as inhibitors of TNF-alpha and IL-6 with antimicrobial activity.
机构信息
Organic Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur 413255, India.
出版信息
Eur J Med Chem. 2010 Jun;45(6):2629-33. doi: 10.1016/j.ejmech.2010.01.050. Epub 2010 Jan 28.
A series of beta-chloro vinyl chalcones have been synthesized by Claisen-Schmidt condensation. beta-chloro vinyl aldehyde has been synthesized by the Vilsmayer-Hack formylation reaction. The structures of the newly synthesized compounds were confirmed by 1H NMR, IR and Mass spectral analysis. All the compounds were evaluated for their anti-inflammatory activity (against TNF-alpha and IL-6) and antimicrobial (antibacterial and antifungal) activity. Compounds 5a, 5d, 5e, 5g and 5i exhibited promising activity against IL-6 with 58-83% inhibition at 10 microM concentration. None of the compound was found to be cytotoxic in CCK-8 cells at 10 microM concentration. Whereas compounds 5b, 5d, 5e and 5i showed very good antibacterial activity and compounds 5a, 5b, 5e and 5i showed good antifungal activity.
通过 Claisen-Schmidt 缩合反应合成了一系列β-氯代乙烯查耳酮。β-氯代乙烯醛通过 Vilsmayer-Hack 甲酰化反应合成。新合成化合物的结构通过 1H NMR、IR 和质谱分析得到确认。所有化合物均评估了其抗炎活性（针对 TNF-α和 IL-6）和抗菌（抗细菌和抗真菌）活性。化合物 5a、5d、5e、5g 和 5i 在 10 μM 浓度下对 IL-6 的抑制率达到 58-83%，表现出有希望的活性。在 10 μM 浓度下，没有一种化合物在 CCK-8 细胞中表现出细胞毒性。而化合物 5b、5d、5e 和 5i 表现出很好的抗菌活性，化合物 5a、5b、5e 和 5i 表现出很好的抗真菌活性。
Zotero 插件