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具有（Z）和（E）-9-[4,4-双（羟甲基）]-2-丁烯基侧链的碳环核苷的合成及生物学评价

Synthesis and biological evaluation of carboacyclic nucleosides with (Z) and (E)-9-[4,4-bis(hydroxymethyl)]-2-butenyl side chain.

作者信息

Tang Ye, Muthyala Ramaiah, Vince Robert

机构信息

Center for Drug Design, Academic Health Center and Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA.

出版信息

Bioorg Med Chem. 2006 Sep 1;14(17):5866-75. doi: 10.1016/j.bmc.2006.05.029. Epub 2006 Jun 8.

DOI:10.1016/j.bmc.2006.05.029
PMID:16759867
Abstract

A series of carboacyclic nucleosides with (Z) and (E)-9-[4,4-bis(hydroxy-methyl)]-2-butenyl side chains were synthesized as ring open analogs of cyclohexene nucleosides 1 and bioisosteres of ganciclovir 3. The (E)-isomers were obtained to compare the side chain geometry effect on antiviral activity.

摘要

合成了一系列带有(Z)和(E)-9-[4,4-双(羟甲基)]-2-丁烯基侧链的碳环核苷，作为环己烯核苷1的开环类似物和更昔洛韦3的生物电子等排体。获得了(E)-异构体以比较侧链几何结构对抗病毒活性的影响。

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