阿昔洛韦和更昔洛韦的荧光三环类似物。结构-抗病毒活性研究。
Fluorescent tricyclic analogues of acyclovir and ganciclovir. A structure-antiviral activity study.
作者信息
Golankiewicz B, Ostrowski T, Goslinski T, Januszczyk P, Zeidler J, Baranowski D, de Clercq E
机构信息
Institute of Bioorganic Chemistry, Polish Academy of Sciences, Noskowskiego 12-14, 61-704 Poznañ, Poland.
出版信息
J Med Chem. 2001 Nov 22;44(24):4284-7. doi: 10.1021/jm010922s.
Of a series of new guanine base modified tricyclic analogues of acyclovir (ACV, 1) and ganciclovir (GCV, 2), derivatives of the 3,9-dihydro-9-oxo-5H-imidazo[1,2-a]purine system, evaluated for activity against herpes simplex virus type 1 and 2, several fluorescent analogues, 6-(4-MeOPh)-TACV (8), 7-Me-6-Ph-TACV (17), 6-(4-MeOPh)-TGCV (27), and 7-Me-6-Ph-TGCV (28), were obtained that showed similar potency and selectivity as the parent compounds. The activity was found to be strongly dependent on the nature and steric demands of the substituents in the 6 and/or 7 position.
在一系列新的阿昔洛韦（ACV，1）和更昔洛韦（GCV，2）的鸟嘌呤碱基修饰的三环类似物中，即3,9 - 二氢 - 9 - 氧代 - 5H - 咪唑并[1,2 - a]嘌呤系统的衍生物，对其抗1型和2型单纯疱疹病毒的活性进行了评估，获得了几种荧光类似物，6 -（4 - 甲氧基苯基）- TACV（8）、7 - 甲基 - 6 - 苯基 - TACV（17）、6 -（4 - 甲氧基苯基）- TGCV（27）和7 - 甲基 - 6 - 苯基 - TGCV（28），它们显示出与母体化合物相似的效力和选择性。发现活性强烈依赖于6位和/或7位取代基的性质和空间需求。
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