含有甲基磺酰基单元的新型乙酰胺衍生化合物的合成与生物活性评估

IF 1.4 4区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR
Pei Li , Zhenchao Wang , Lei Yu
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引用次数: 0

摘要

本研究报告了一系列含有甲磺酰基单元的新型乙酰胺衍生化合物的合成和结构表征。体外抗菌活性结果表明,化合物 2-((4-氟苯基)磺酰基)-N-(4-(甲基磺酰基)苯基)乙酰胺 (6b) 对黄单胞菌 oryzae pv.oryzicolaby(Xoc)、Xanthomonas oryzae pv. oryzae(Xoo)和 Xanthomonas axonopodis pv. citri(Xac)的抗菌活性,与 Bismerthiazol 和 Thiodiazole copper 相比,在 100 μg/mL 浓度下的抑制率分别为 86.24%、81.59% 和 75.65%。同时发现,与多菌灵相比,所有目标化合物在 50 μg/mL 浓度下对脆弱拟南芥(M. fragilis)、贝氏拟南芥(M. bainieri)和阿特罗维里德毛霉(T. atroviride)的体外抗真菌活性均较低,抑制率分别为 0-45.21%、0-30.24% 和 0-12.65%。此外,目标化合物在 10 μM 浓度下对前列腺癌(PC3)、肝癌(HepG2)和白血病(K562)细胞的生物测定结果表明,与 5-氟尿嘧啶相比,化合物 2-((4-氟苯基)硫)-N-(4-(甲磺酰基)苯基)乙酰胺(4c)对 K562 具有明显的抗肿瘤活性(56.87%)。这项工作首次强调了带有甲磺酰基单元的乙酰胺衍生化合物的修饰对生物活性评估的影响。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis and bioactivity evaluation of novel acetamide-derived compounds bearing a methylsulfonyl unit

This study reports the synthesis and structural characterization of a series of novel acetamide-derived compounds containing a methylsulfonyl unit. The in vitro antibacterial activity results demonstrated that compound 2-((4-fluorophenyl)sulfonyl)-N-(4-(methylsulfonyl)phenyl)acetamide (6b) exhibited superior antibacterial activities against Xanthomonas oryzae pv. oryzicolaby (Xoc), Xanthomonas oryzae pv. oryzae (Xoo), and Xanthomonas axonopodis pv. citri (Xac) at 100 μg/mL concentration, with the inhibition rates of 86.24%, 81.59%, and 75.65%, respectively, compared to Bismerthiazol and Thiodiazole copper. Meanwhile, the in vitro antifungal activities of all target compounds were found to be lower against Mucor fragilis (M. fragilis), Mucor bainieri (M. bainieri), and Trichoderma atroviride (T. atroviride) at 50 μg/mL concentration, with the inhibition rates of 0–45.21%, 0–30.24%, and 0–12.65%, respectively, compared to Carbendazim. Moreover, bioassay results of the target compounds against prostate cancer (PC3), hepatocellular carcinoma (HepG2), and leukemia (K562) cells at 10 μM concentration demonstrated that, compared to 5-fluorouracil, compound 2-((4-fluorophenyl)thio)-N-(4-(methylsulfonyl)phenyl)acetamide (4c) illustrated obvious antitumor activity (56.87%) against K562. This work first highlights the effect of the modification of the acetamide-derived compounds bearing a methylsulfonyl unit on the bioactivity evaluation.

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来源期刊
CiteScore
2.60
自引率
7.70%
发文量
103
审稿时长
2.1 months
期刊介绍: Phosphorus, Sulfur, and Silicon and the Related Elements is a monthly publication intended to disseminate current trends and novel methods to those working in the broad and interdisciplinary field of heteroatom chemistry.
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