Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2013-11-16 , DOI: 10.1016/j.bmcl.2013.11.009 Wen Gu , Chao Qiao , Shi-Fa Wang , Yun Hao , Ting-Ting Miao
A series of new N-substituted 1H-dibenzo[a,c]carbazole derivatives were synthesized from dehydroabietic acid, and their structures were characterized by IR, 1H NMR and HRMS spectral data. All compounds were evaluated for their antibacterial and antifungal activities against four bacteria (Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas fluorescens) and three fungi (Candida albicans, Candida tropicalis and Aspergillus niger) by serial dilution technique. Some of the synthesized compounds displayed pronounced antimicrobial activity against tested strains with low MIC values ranging from 0.9 to 15.6 μg/ml. Among them, compounds 6j and 6r exhibited potent inhibitory activity comparable to reference drugs amikacin and ketoconazole.
中文翻译:
新型脱氢松香酸的N-取代的1 H-二苯并[ a,c ]咔唑衍生物的合成及生物学评价
由脱氢松香酸合成了一系列新的N-取代的1H-二苯并[ a,c ]咔唑衍生物,并通过IR,1 H NMR和HRMS光谱数据对其结构进行了表征。评估了所有化合物对四种细菌(枯草芽孢杆菌,金黄色葡萄球菌,大肠杆菌和荧光假单胞菌)和三种真菌(白色念珠菌,热带念珠菌和黑曲霉)的抗菌和抗真菌活性。)通过系列稀释技术。一些合成的化合物显示出对受测菌株具有显着的抗菌活性,MIC值介于0.9至15.6μg/ ml之间。其中,化合物6j和6r表现出与参考药物阿米卡星和酮康唑相当的有效抑制活性。