Department of Chemistry, University School of Sciences, Gujarat University , Ahmedabad, Gujarat , India , and.
J Enzyme Inhib Med Chem. 2014 Feb;29(1):100-8. doi: 10.3109/14756366.2012.755622. Epub 2013 Jan 18.
A series of novel hybrid quinazoline-triazine derivatives was designed and synthesized from cyanuric chloride and anthranilic acid through sequential reactions, which contain different pharmacophores like quinazoline and substituted diaryl triazine (DATA) linked with ethylene diamine. All the newly synthesized compounds were characterized by infrared, (1)H-NMR, (13)C-NMR, MS and elemental analysis. Further, we evaluated the in vitro anti-HIV activity of the newly synthesized compounds against HIV-1 (IIIB) and HIV-2 (ROD) viral strains and as well as in vitro antimicrobial activity against four bacteria (Staphylococcus aureus, Bacillus cereus, Pseudomonas aeruginosa, Klebsiella pneumoniae) and two fungi (Aspergillus clavatus, Candida albicans) using the paper agar streak dilution method. The bioassay results indicate that four compounds namely 7d, 7n, 7r and 7s could be considered as possible potential agents.
设计并合成了一系列新型的杂化喹唑啉-三嗪衍生物，该衍生物是由三聚氯氰和邻氨基苯甲酸经连续反应得到的，其中包含不同的药效团，如喹唑啉和取代的二芳基三嗪（DATA）与乙二胺相连。所有新合成的化合物均通过红外、（1）H-NMR、（13）C-NMR、MS 和元素分析进行了表征。此外，我们还采用纸片琼脂扩散稀释法评估了新合成化合物对 HIV-1（IIIb）和 HIV-2（ROD）病毒株的体外抗 HIV 活性以及对四种细菌（金黄色葡萄球菌、蜡样芽孢杆菌、铜绿假单胞菌、肺炎克雷伯菌）和两种真菌（构巢曲霉、白色念珠菌）的体外抗菌活性。生物测定结果表明，有四个化合物，即 7d、7n、7r 和 7s，可被视为有潜力的候选药物。
