Anthem Biosciences Pvt. Ltd, No. 49, Bommasandra Industrial Area, Bommasandra, Bangalore 560099, Karnataka, India.
Eur J Med Chem. 2010 Sep;45(9):3803-10. doi: 10.1016/j.ejmech.2010.05.030. Epub 2010 May 20.
A new series of [1-(6-methoxy-2-methylquinolin-4-yl)-1H-1,2,3-triazol-4-yl] methanamine derivatives were synthesized starting from 4-methoxyaniline through multi-step reactions. The title compounds 5a-y were prepared by treating the azide intermediate 4 with propargyl bromide and different alkyl/heterocyclic amines in a sequential three component synthesis. All the new compounds were characterized by spectral and elemental analyses. The newly synthesized final compounds were evaluated for their in vitro antibacterial and antifungal activities against pathogenic strains. The preliminary screening results indicated that most of the compounds demonstrated moderate to very good antibacterial and antifungal activities, comparable to the first-line drugs.
以 4-甲氧基苯胺为起始原料，经多步反应合成了一系列新型的[1-(6-甲氧基-2-甲基喹啉-4-基)-1H-1,2,3-三唑-4-基]甲胺衍生物。通过将叠氮化物中间体 4 与丙炔溴和不同的烷基/杂环胺在连续三组分合成中进行反应，制备了标题化合物 5a-y。所有新化合物均通过光谱和元素分析进行了表征。新合成的最终化合物进行了体外抗菌和抗真菌活性评估，以对抗致病菌。初步筛选结果表明，大多数化合物表现出中等至非常好的抗菌和抗真菌活性，可与一线药物相媲美。
