Design and synthesis of acyclic nucleoside analogs with chlorinated imidazo[1,2-a]pyridine bases.
Design and synthesis of acyclic nucleoside analogs with chlorinated imidazo[1,2-a]pyridine bases.
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具有氯化咪唑并[1,2-a]吡啶碱基的无环核苷类似物的设计和合成。
DOI：
10.1081/ncn-120025238
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发表时间：
2003
期刊：
影响因子：
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通讯作者：
Townsend,LeroyB
中科院分区：
文献类型：
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作者：
Williams,JohnD;Mourad,AlaaE;Drach,JohnC;Townsend,LeroyB
合成了一系列2，6-二氯和2，6，7-三氯咪唑并[1，2-a]吡啶的无环C-核苷类似物，并进行了抗病毒活性测试。将适当的羟甲基取代的杂环依次用亚硫酰氯、适当的亲核试剂、然后用二异丙基乙胺处理，以获得所需的无环核苷类似物。评价了这些化合物对人巨细胞病毒和单纯疱疹病毒1型的活性。在非细胞毒性浓度下，两种二氯类似物显示出轻微的抗病毒活性（IC 50 = 20-45 µM），但三氯类似物均未显示出轻微的抗病毒活性。
A series of acyclic C-nucleoside analogs of 2,6-dichloro- and 2,6,7-trichloroimidazo[1,2-a]pyridine were synthesized and tested for antiviral activity. The appropriate hydroxymethyl-substituted heterocycles were treated successively with thionyl chloride, an appropriate nucleophile, then diisopropylethylamine to obtain the desired acyclic nucleoside analogs. These compounds were evaluated for activity against human cytomegalovirus and herpes simplex virus, type 1. Two of the dichloro analogs, but none of the trichloro analogs demonstrated slight antiviral activity (IC50's = 20–45 µM) at non-cytotoxic concentrations.