2'-脱氧-4'-硫代嘧啶核苷的合成及其抗疱疹病毒活性
Synthesis and anti-herpes virus activity of 2'-deoxy-4'-thiopyrimidine nucleosides.
作者信息
Rahim S G, Trivedi N, Bogunovic-Batchelor M V, Hardy G W, Mills G, Selway J W, Snowden W, Littler E, Coe P L, Basnak I, Whale R F, Walker R T
机构信息
Wellcome Research Laboratories, Beckenham, Kent, U.K.
出版信息
J Med Chem. 1996 Feb 2;39(3):789-95. doi: 10.1021/jm950029r.
A series of 5-substituted 2'-deoxy-4'-thiopyrimidine nucleosides was synthesized and evaluated as potential antiviral agents. A number of analogues such as 2'-deoxy-5-propyl-4'-thiouridine (3ii), 2'-deoxy-5-isopropyl-4'-thiouridine (3iii), 5-cyclopropyl-2'-deoxy-4'-thiouridine (3iv), 2'-deoxy-4'-thio-5-vinyluridine (3viii), and 5-(2-chloroethyl)-2'-deoxy-4'-thiouridine (3xx) were found to be highly active against herpes simplex virus type-1 (HSV-1) and varicella zoster virus (VZV) in vitro with no significant cytotoxicity. The compound with the broadest spectrum of activity was 2'-deoxy-5-ethyl-4'-thiouridine (3i) which showed significant activity against HSV-1, HSV-2, and VZV.
合成了一系列5-取代的2'-脱氧-4'-硫代嘧啶核苷，并将其作为潜在的抗病毒药物进行评估。发现许多类似物，如2'-脱氧-5-丙基-4'-硫代尿苷（3ii）、2'-脱氧-5-异丙基-4'-硫代尿苷（3iii）、5-环丙基-2'-脱氧-4'-硫代尿苷（3iv）、2'-脱氧-4'-硫代-5-乙烯基尿苷（3viii）和5-(2-氯乙基)-2'-脱氧-4'-硫代尿苷（3xx）在体外对单纯疱疹病毒1型（HSV-1）和水痘带状疱疹病毒（VZV）具有高活性，且无明显细胞毒性。活性谱最广的化合物是2'-脱氧-5-乙基-4'-硫代尿苷（3i），它对HSV-1、HSV-2和VZV均表现出显著活性。
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