一些核苷类似物的合成与抗病毒活性
Synthesis and anti-virus activity of some nucleosides analogues.
作者信息
Stankova I G, Simeonov M F, Maximova V, Galabov A S, Golovinsky E V
机构信息
Department of Chemistry, South-West University Neofit Rilski, Blagoevgrad, Bulgaria.
出版信息
Z Naturforsch C J Biosci. 1999 Jan-Feb;54(1-2):75-83.
New 3'-, 5'-, 5-bromo-2'-deoxyuridine (3a-g) and 3'-, 5'-thymidine (4a-i) analogues with amino acid and peptide residues were synthesized and evaluated for antiviral activity. The influence of long peptide chains, essential amino acids and the effect of this structural modification on the antiviral activity has been also reported. Three 5-bromo-2'-deoxyuridine derivatives containing glycyl-, glycyl-glycyl- and glycyl-glycyl-glycyl- residues (3a, 3b, 3c) showed a strong activity against the herpes virus PsRV and a moderate one vs. HSV-1. The corresponding thymidine analogues were considerably less effective, and only compounds 4d and 4h showed a borderline effect against PsRV.
合成了带有氨基酸和肽残基的新型3′-、5′-、5-溴-2′-脱氧尿苷（3a - g）和3′-、5′-胸苷（4a - i）类似物，并对其抗病毒活性进行了评估。还报道了长肽链、必需氨基酸的影响以及这种结构修饰对抗病毒活性的作用。三种含有甘氨酰基、甘氨酰 - 甘氨酰基和甘氨酰 - 甘氨酰 - 甘氨酰基残基的5-溴-2′-脱氧尿苷衍生物（3a、3b、3c）对疱疹病毒PsRV表现出强活性，对单纯疱疹病毒1型（HSV - 1）表现出中等活性。相应的胸苷类似物效果要差得多，只有化合物4d和4h对PsRV表现出临界效应。
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