Molecular hybridization approach is an emerging tool in drug discovery for designing new pharmacophores with biological activity. A novel, new series of coumarin–benzimidazole hybrids were designed, synthesized and evaluated for their broad spectrum antimicrobial activity. Among all the synthesized molecules, compound (E)-3-(2-1H-benzo[d]imidazol-1-yl)-1-((4-chlorobenzyl)oxy)imino)ethyl)-2H-chromen-2-one showed the most promising broad spectrum antibacterial activity against Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis and Proteus vulgaris. In addition, it has showed no cytotoxicity and hemolysis at 10 times the MIC concentration. SAR studies indicate that position of the chlorine atom in the hybrid critically determines the antibacterial activity.

中文翻译：

---

香豆素-苯并咪唑杂种作为有效的抗菌剂：合成和生物学提升

分子杂交方法是用于开发具有生物活性的新药效基团的药物发现中的新兴工具。设计，合成和评估了香豆素-苯并咪唑杂物的新系列，并对其广谱抗菌活性进行了评估。在所有合成的分子中，化合物（E）-3-（2-1H-苯并[ d ]咪唑-1-基）-1-（（4-氯苄基氧基）亚氨基）乙基）-2H-铬-2-一种对铜绿假单胞菌，金黄色葡萄球菌，枯草芽孢杆菌和寻常变形杆菌具有最有前景的广谱抗菌活性。此外，在MIC浓度的10倍时，它没有显示出细胞毒性和溶血作用。SAR研究表明，杂化物中氯原子的位置决定了抗菌活性。