Department of Chemistry, faculty of Science, Taif University, Taif 21974, Saudi Arabia.
Department of Biochemistry, Faculty of Agriculture, Cairo University, Giza 12613, Egypt.
Molecules. 2018 Dec 11;23(12):3285. doi: 10.3390/molecules23123285.
The paper describes the synthesis and biological evaluation of some new benzimidazole derivatives as potent clinical drugs that are useful in the treatment of some microbial infections and tumor inhibition. The starting compound 2-(bromomethyl)-1-benzimidazole () was prepared, and hence underwent interesting functionalization reactions to afford several series of benzimidazole-5-(aryldiazenyl)thiazole derivatives: ⁻, ⁻, and ⁻. The antibacterial activities of the synthesized compounds were evaluated by calculation of the inhibition zone diameter (mm) and the determination of minimum inhibitory concentration (µg/mL) against selected pathogenic bacteria (Gram-positive bacteria) and (Gram-negative bacteria).Noticeable efficiency was found based on in vitro screening for their antioxidant activity and cytotoxicity effect against the human liver cancer cell line (HepG2) and human hepatocyte carcinoma cells at relatively high concentrations.
本文描述了一些新型苯并咪唑衍生物的合成和生物评价，这些衍生物作为有效的临床药物，可用于治疗某些微生物感染和肿瘤抑制。以起始化合物 2-(溴甲基)-1-苯并咪唑（）为原料，通过有趣的功能化反应，得到了几系列苯并咪唑-5-（芳基亚氨基）噻唑衍生物：、和。通过计算抑菌圈直径（mm）和最小抑菌浓度（µg/mL）来评估合成化合物对选定致病菌（革兰氏阳性菌）和（革兰氏阴性菌）的抗菌活性。根据体外筛选，这些化合物在相对较高浓度下对人肝癌细胞系（HepG2）和人肝癌细胞具有抗氧化活性和细胞毒性作用，表现出显著的效率。
