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首页> 外文期刊>Pharmaceutical Chemistry Journal >THE SEARCH FOR NEW THERAPEUTIC AGENTS SYNTHESIS OF ANIONIC DERIVATIVES OF MFO-INOSITOL AND OTHER POLYOLS AND INVESTIGATION OF THEIR ANTIVIRAL ACTIVITY
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THE SEARCH FOR NEW THERAPEUTIC AGENTS SYNTHESIS OF ANIONIC DERIVATIVES OF MFO-INOSITOL AND OTHER POLYOLS AND INVESTIGATION OF THEIR ANTIVIRAL ACTIVITY

机译:MFO-肌醇和其他多羟基化合物阴离子衍生物的新治疗剂合成及其抗病毒活性的研究

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The search for new, effective antiviral agents currently includes assessment of polyanionic compounds of various structures; these are highly active inhibitors of viral penetration into cells. The present report describes the preparation of phosphate and sulfate derivatives based on 2,3,4,5-tetra-O-benzyl-D,?-iditol, 1,12-dodecanediol, and a dimeric analog of inositol-containing phospholipids. The dimeric derivative, which contains two myo-inositol cyclitol rings linked by a single hydrophobic fragment, was synthesized at high yield using the H-phosphonate method. The antiviral activity of the series of compounds synthesized here was assessed against a panel of viruses. All were inactive against rhinoviruses; the disulfate of tetra-O-benzyl-D, i-iditol inhibited Coxsackie virus and had the greatest cytotoxicity; the disulfate of 1,2-dodecanediol was inactive against all viruses, while the diphosphate of 2,3,4,5-tetra-O-benzyl-A?-iditol and the monosulfate of 1,2-dodecanediol were active against herpes simplex viruses types 1 and 2.
机译:目前,寻找新的有效抗病毒药的方法包括评估各种结构的聚阴离子化合物。这些是病毒渗入细胞的高效抑制剂。本报告描述了基于2,3,4,5-四-O-苄基-D,α-ID醇,1,12-十二烷二醇和含肌醇磷脂的二聚体类似物的磷酸盐和硫酸盐衍生物的制备。使用H-膦酸酯方法以高收率合成了二聚体衍生物,该衍生物包含两个通过单个疏水性片段连接的肌醇-环醇环。对一组病毒评估了此处合成的一系列化合物的抗病毒活性。所有的人都没有针对鼻病毒的活性;四-O-苄基-D,异-糖醇的二硫酸盐抑制了柯萨奇病毒,并具有最大的细胞毒性。 1,2-十二烷二醇的二硫酸盐对所有病毒均无活性,而2,3,4,5-四-O-苄基-Aβ-糖醇的二磷酸酯和1,2-十二烷二醇的单硫酸盐对单纯疱疹有活性。 1型和2型病毒。

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