3-氨基-1,2,4-三唑-5-硫酸盐新型席夫碱的设计、合成、表征及作为抗菌药物的生物学评价

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引用次数: 0

摘要

以不同的苯甲醛衍生物为原料,在啉存在下与3-氨基-1,2,4-三唑-5-硫醇反应制备了希夫碱(T1-T10),并利用紫外光谱、FIR光谱、GC-Mass、1H-NMR对所制备的化合物进行了表征,并测定了其熔点。所得结果证实了所制备化合物结构的有效性。所有化合物(T1-T10)对4种革兰氏阳性菌和革兰氏阴性菌的生物活性进行了测试。研究表明,化合物T8对金黄色葡萄球菌的抑制作用IC50值为22µg/mL,其次是T1、T10、T2和T3, IC50值分别为25、26、33和33µg/mL。T3、T10、T2、T1、T4对铜绿假单胞菌均有抑制作用,IC50值分别为22、28、39、44、50µg/mL。T4、T2、T5对变形链球菌的抑制作用IC50值分别为28、32、38µg/mL。有趣的是,T6对肺炎克雷伯菌的抑制作用最强,IC50为15µg/mL。本研究结果提示,T8、T3、T4和T6可能是治疗金黄色葡萄球菌、铜绿假单胞菌、变形链球菌和肺炎克雷伯菌的潜在新型抗生素。然而,需要进一步的研究来证实这些发现,并评估这些化合物在人体中的安全性和有效性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Design, Synthesis, And Characterization Of New Schiff Bases For 3-Amino-1,2,4-Triazole-5-Thiolate Salt, Bearing Morpholine Ring And Biological Evaluation As Antibacterial Agents
Schiff bases (T1-T10) were prepared from the reaction of various benzaldehyde derivatives with 3-amino-1,2,4-triazole-5-thiol in the presence of Morpholine, and all the prepared compounds were characterized using UV, FIR spectroscopy, in addition to GC-Mass, 1H-NMR for some combinations and measuring their melting points. The obtained results confirmed the validity of the proposed structures of the prepared compounds. The biological activity of all prepared compounds (T1-T10) was tested against four types of Gram-positive and Gram-negative bacteria. The study showed that the compound T8 inhibited Staphylococcus aureus with an IC50 of 22 µg/mL, followed by T1, T10, T2, and T3 with IC50 values of 25, 26, 33, and 33 µg/mL, respectively. In addition, T3, T10, T2, T1, and T4 had an inhibitory effect on Pseudomonas aeruginosa with IC50 values of 22, 28, 39, 44, and 50 µg/mL, respectively. T4, T2, and T5 inhibited Streptococcus mutans with IC50 values of 28, 32, and 38 µg/mL, respectively. Interestingly, T6 had the strongest inhibitory effect on Klebsiella pneumoniae with an IC50 of 15 µg/mL. The results of this study suggest that T8, T3, T4, and T6 may be potential new antibiotics for the treatment of Staphylococcus aureus, Pseudomonas aeruginosa, Streptococcus mutans, and Klebsiella pneumoniae. However, further studies are needed to confirm these findings and to evaluate the safety and efficacy of these compounds in humans.
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