Synthesis, antimicrobial, antioxidant, anti-hemolytic and cytotoxic evaluation of new imidazole-based heterocycles

被引:139
作者
Abdel-Wahab, Bakr F. [1 ,2 ]
Awad, Ghada E. A.
Badria, Farid A. [3 ]
机构
[1] King Abdel Aziz Univ, Dept Chem, Fac Sci & Arts, Khulais Branch, Jeddah, Saudi Arabia
[2] Natl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
[3] Mansoura Univ, Dept Pharmacognosy, Fac Pharm, Mansoura 35516, Egypt
关键词
Imidazole; Thiazoles; Hydrazonoyl chlorides; Antimicrobial; antioxidant; anti-hemolytic; cytotoxic; DERIVATIVES; ANALOGS; DESIGN; ETHERS;
D O I
10.1016/j.ejmech.2011.01.062
中图分类号
R914 [药物化学];
学科分类号
100701 ;
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 mu g/mL While, compounds 2, 8 and 10a were the best antioxidant reagents using the DPPH method. Compounds 6a and 10b proved to exhibit potent anti-oxidative 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. (C) 2011 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:1505 / 1511
页数:7
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