АBSTRACT Esters of the antiherpetic drugs ganciclovir, penciclovir with the bile acids (cholic, chenodeoxycholic and deoxycholic) and amino acid esters of acyclovir were generated and evaluated for their in vitro antiviral activity against herpes simplex viruses type 1 and type 2 (HSV-1, HSV-2). The antiviral assays demonstrated that modified analogs of ACV and PCV are less active compared to the initial substances against HSV-1and HSV-2. CC50 for ganciclovir-deoxycholate corresponded to the CC50 of the other analogs and its activity is lower than ganciclovir. Obtained results show that tested modification do not improve bioavailability of nucleoside analogs in cells.

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更昔洛韦、喷昔洛韦、阿昔洛韦的杂环碱基的修饰 - 合成和抗病毒特性

АBSTRACT 抗疱疹药物更昔洛韦、喷昔洛韦与胆汁酸（胆酸、鹅去氧胆酸和脱氧胆酸）的酯和阿昔洛韦的氨基酸酯被生成并评估了它们对 1 型和 2 型单纯疱疹病毒（HSV-1， HSV-2）。抗病毒试验表明，与抗 HSV-1 和 HSV-2 的初始物质相比，ACV 和 PCV 的修饰类似物活性较低。更昔洛韦-脱氧胆酸盐的CC50对应于其他类似物的CC50，其活性低于更昔洛韦。获得的结果表明，测试的修饰不会提高细胞中核苷类似物的生物利用度。