Chemistry Department, Faculty of Science and Arts, King Abdel-Aziz University, Khulais Branch, Saudi Arabia.
Eur J Med Chem. 2011 May;46(5):1505-11. doi: 10.1016/j.ejmech.2011.01.062. Epub 2011 Feb 3.
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 μg/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.
在本工作中，制备了 1-(5-甲基-2-苯基-1H-咪唑-4-基)乙酮 1，并将其用作合成新噻唑、芳亚基和香豆素衍生物的前体。对新化合物的抗菌、抗氧化、抗溶血和细胞毒性活性进行了筛选。化合物 12 对所有测试的细菌均表现出优异的抗菌活性，最小抑菌浓度 (MIC) 范围在 21.9 至 43.8μg/mL 之间。而，化合物 2、8 和 10a 是使用 DPPH 法的最佳抗氧化试剂。化合物 6a 和 10b 被证明具有很强的抗氧化活性，表现在抑制大鼠脑和肾匀浆中脂质过氧化以及红细胞溶血的能力。在体外艾氏腹水试验中，化合物 6a 表现出最高的细胞毒性活性（81.9%），其次是 2、6c、7b 和 12。详细的合成方法、光谱数据和生物结果都有记录。
