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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, antimicrobial, antioxidant, anti-hemolytic and cytotoxic evaluation of new imidazole-based heterocycles.
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Synthesis, antimicrobial, antioxidant, anti-hemolytic and cytotoxic evaluation of new imidazole-based heterocycles.

机译:新咪唑基杂环的合成,抗菌,抗氧化剂,抗溶血和细胞毒性评估。

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摘要

In the present work, 1-(5-methyl-2-phenyl-1H-imidazol-4-yl)ethanone 1 was prepared and used as a precursor for the synthesis of new thiazole, arylidiene and coumarin derivatives. The antimicrobial, antioxidant, anti-hemolytic, and cytotoxic activities of new compounds have been screened. Compound 12 showed an excellent antibacterial activity for all the tested bacteria with minimal inhibitory concentration (MIC) ranged between 21.9 and 43.8 mug/mL. While, compounds 2, 8 and 10a were the best antioxidant reagents using the DPPH method. Compounds 6a and 10b proved to exhibit potent antioxidative activity as reflected in the ability to inhibit lipid per-oxidation in rat brain and kidney homogenates and rate erythrocyte hemolysis. Compounds 6a proved to have the highest cytotoxic activity (81.9%) followed by 2, 6c, 7b and 12 using in vitro Ehrlich ascites assay. The details synthetic methods, spectroscopic data and biological results are recorded.
机译:在本工作中,制备了1-(5-甲基-2-苯基-1H-咪唑-4-基)乙酮1,并用作合成新的噻唑,芳基二烯和香豆素衍生物的前体。已经筛选了新化合物的抗微生物,抗氧化剂,抗溶血和细胞毒性活性。化合物12对所有测试细菌均表现出优异的抗菌活性,最小抑菌浓度(MIC)在21.9和43.8马克杯/毫升之间。同时,使用DPPH方法,化合物2、8和10a是最好的抗氧化剂。化合物6a和10b被证明具有强大的抗氧化活性,这表现在抑制大鼠脑和肾脏匀浆中脂质过氧化的能力以及对红细胞溶血速率的反映。使用体外Ehrlich腹水分析,化合物6a被证明具有最高的细胞毒活性(81.9%),其次是2、6c,7b和12。记录详细的合成方法,光谱数据和生物学结果。

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