Robins M J, Hatfield P W, Balzarini J, De Clercq E
J Med Chem. 1984 Nov;27(11):1486-92. doi: 10.1021/jm00377a018.
Various acyclic, i.e., (2-hydroxyethoxy)methyl and (2-acetoxyethoxy)methyl, analogues of pyrimidine and purine nucleosides have been prepared and evaluated for their antiviral, antimetabolic, and cytotoxic properties. All of the pyrimidine analogues, including (E)-5-(2-bromovinyl)-1-[(2-hydroxyethoxy)methyl]uracil (12) and its O-acetyl derivative (13), were virtually devoid of antiviral, cytotoxic, and antimetabolic activities. However, several of the 8-substituted derivatives of 9-[(2-hydroxyethoxy)methyl]guanine (acyclovir) had higher antiviral specificity in vitro than the parent drug. The 8-methyl-, 8-amino-, 8-bromo-, and 8-iodoacyclovir derivatives have activities worthy of further investigation.
已制备了各种无环的，即（2-羟基乙氧基）甲基和（2-乙酰氧基乙氧基）甲基的嘧啶和嘌呤核苷类似物，并对其抗病毒、抗代谢和细胞毒性特性进行了评估。所有嘧啶类似物，包括（E）-5-（2-溴乙烯基）-1-[(2-羟基乙氧基）甲基]尿嘧啶（12）及其O-乙酰基衍生物（13），实际上都没有抗病毒、细胞毒性和抗代谢活性。然而，9-[(2-羟基乙氧基）甲基]鸟嘌呤（阿昔洛韦）的几种8-取代衍生物在体外具有比母体药物更高的抗病毒特异性。8-甲基-、8-氨基-、8-溴-和8-碘阿昔洛韦衍生物具有值得进一步研究的活性。
