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某些糖芳基甘氨酰腙及其恶二唑啉衍生物的合成与抗病毒活性评价

Synthesis and antiviral evaluation of some sugar arylglycinoylhydrazones and their oxadiazoline derivatives.

作者信息

Abdel-Aal Mohammed T, El-Sayed Wael A, El-Ashry El-Sayed H

机构信息

Photochemistry Department, National Research Centre, Cairo, Egypt.

出版信息

Arch Pharm (Weinheim). 2006 Dec;339(12):656-63. doi: 10.1002/ardp.200600100.

Abstract

Sugar N-arylaminoacetylhydrazones 2-5 were prepared by the reaction of N-arylaminoacetylhydrazides 1 with equivalent amounts of the corresponding monosaccharides. Per-O-acetyl derivatives 6-9 of sugar hydrazones 2-5 were prepared by using acetic anhydride in pyridine at room temperature, while on boiling with acetic anhydride, cyclization had taken place to give the oxadiazolines 10-12. The prepared compounds were tested for antiviral activity against Herpes Simplex virus type-1 (HSV-1) and hepatitis-A virus (HAV, MBB-cell culture adapted strain). Plaque reduction infectivity assay was used to determine virus count reduction as a result of treatment with tested compounds.

摘要

糖N-芳基氨基乙酰腙2-5是通过N-芳基氨基乙酰肼1与等量相应单糖反应制备的。糖腙2-5的全-O-乙酰基衍生物6-9是在室温下于吡啶中使用乙酸酐制备的,而在与乙酸酐一起煮沸时发生环化反应生成恶二唑啉10-12。对所制备的化合物进行了针对1型单纯疱疹病毒(HSV-1)和甲型肝炎病毒(HAV,MBB细胞培养适应株)的抗病毒活性测试。采用噬斑减少感染性测定法来确定经测试化合物处理后病毒数量的减少情况。

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