Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Al-Azhar University, Cairo, Egypt.
Arch Pharm (Weinheim). 2017 May;350(5). doi: 10.1002/ardp.201700028. Epub 2017 Apr 13.
Ethyl (6,7-dimethyl-2-oxo-3,4-dihydroquinoxalin-3-yl)acetate and ethyl (6-methyl-2-oxo-3,4-dihydroquinoxalin-3-yl)acetate (1a,b), 3-methylquinoxalin-2(1H)-one (4) and 1,4-dihydroquinoxaline-2,3-dione (11) were the starting precursors for nine novel quinoxaline compounds, 3a, 6, 10, 13, 15, 16, 17, 18, and 20, via adopting different nucleophilic reactions. The synthesized compounds were tested for their antiviral activity against HCV, HBV, HSV-1, and HCMV. Concomitantly, their safety profile was investigated as well as their selectivity against the viral strains. The Virology Unit at the University of Alabama recorded that two compounds, i.e., 1a and 20, exhibited highly potent activity against HCMV with lower IC values (<0.05 μM) compared to ganciclovir (IC = 0.59 μM). Compounds 1a and 20 also exhibited low cytotoxicity together with a high selectivity index.
乙酯（6,7-二甲基-2-氧代-3,4-二氢喹喔啉-3-基）和乙酯（6-甲基-2-氧代-3,4-二氢喹喔啉-3-基）（1a,b）、3-甲基喹喔啉-2（1H）-酮（4）和 1,4-二氢喹喔啉-2,3-二酮（11）是通过采用不同的亲核反应合成 9 种新型喹喔啉化合物 3a、6、10、13、15、16、17、18 和 20 的起始前体。合成的化合物被测试其对 HCV、HBV、HSV-1 和 HCMV 的抗病毒活性。同时，还研究了它们的安全性特征以及对病毒株的选择性。阿拉巴马大学的病毒学部门记录到，两种化合物 1a 和 20 对 HCMV 表现出高度有效的活性，其 IC 值（<0.05μM）低于更昔洛韦（IC = 0.59μM）。化合物 1a 和 20 还表现出低细胞毒性和高选择性指数。
