Department of Chemistry, University of Jammu, Jammu 180 006, India.
Bioorg Med Chem Lett. 2011 Aug 15;21(16):4919-23. doi: 10.1016/j.bmcl.2011.06.007. Epub 2011 Jun 17.
The title compounds, 9-substituted-3-aryl-5H,13aH-quinolino[3,2-f][1,2,4]triazolo[4,3-b][1,2,4]triazepines 8, are synthesized from 5-aryl-3,4-diamino-1,2,4-triazoles 5 and 2-chloro-3-formylquinolines 7 in ionic liquid as solvent under microwave heating as well as using oil-bath heating at 80°C. The products are obtained in the good to moderate yields and in high purity. These compounds have been screened for antifungal activity. The screening data indicate that the compounds 8a, 8b, 8c and 8d show excellent activity against Aspergillus niger 1000 μg concentration and Pencillium notatum species at 500 μg as well as 1000 μg concentrations whereas, these compounds show good to moderate activity against Aspergillus flavus and Rhizopus species at both the concentrations. Moreover, ionic liquid is found to be recyclable for at least three consecutive runs what makes the process cost-effective and economic that lead to the area of Green Chemistry as recyclability is one of the most important feature of Green Chemistry.
标题化合物，9-取代-3-芳基-5H,13aH-喹啉并[3,2-f][1,2,4]三唑并[4,3-b][1,2,4]三嗪 8，是由 5-芳基-3,4-二氨基-1,2,4-三唑 5 和 2-氯-3-甲酰基喹啉 7 在离子液体溶剂中微波加热以及在 80°C 油浴加热下合成的。这些产物以良好到中等的产率和高纯度获得。这些化合物已经被筛选出具有抗真菌活性。筛选数据表明，化合物 8a、8b、8c 和 8d 对黑曲霉 1000μg 浓度和青霉属物种在 500μg 和 1000μg 浓度下表现出优异的活性，而这些化合物在两种浓度下对黄曲霉和根霉属物种表现出良好到中等的活性。此外，发现离子液体至少可连续回收使用三次，这使得该过程具有成本效益和经济性，从而推动了绿色化学领域的发展，因为可回收性是绿色化学的最重要特征之一。
