含氟和硫取代基的无环核苷的合成及其抗病毒活性评估。

Synthesis and evaluation of the antiviral activity of acyclic nucleosides carrying fluorine and sulfur substituents.

作者信息

Bravo P, Resnati G, Viani F, De Montis A, Corrias S, La Colla P

机构信息

Dipartimento di Chimica, Politecnico, Milano, Italy.

出版信息

Farmaco. 1993 Aug;48(8):1113-20.

PMID:8216673

Abstract

-2',3'-Seco nucleosides 5 carrying fluorine and sulfur substituents at C-3' and C-5', respectively, of acyclic sugar moiety were synthesized in enantiomerically and diastereoisomerically pure form. These products and some structurally similar 1',2'-seco-2'-nor-and 1',2'-seco-nucleosides 3 and 4 were tested in vitro for cytotoxicity and antiviral activity. At non-cytotoxic concentrations the compounds were inactive against human immunodeficiency virus and herpes simplex virus type-1.

摘要

分别在无环糖部分的C-3'和C-5'位带有氟和硫取代基的-2',3'-开环核苷5以对映体纯和非对映体纯的形式合成。对这些产物以及一些结构相似的1',2'-开环-2'-去甲核苷3和1',2'-开环核苷4进行了体外细胞毒性和抗病毒活性测试。在无细胞毒性浓度下，这些化合物对人类免疫缺陷病毒和1型单纯疱疹病毒无活性。