新合成硫代糖苷及其开链类似物的抗病毒和抗血吸虫活性评估
Antiviral and antischistosomal evaluation of newly synthesized thioglycosides and their acyclic analogues.
作者信息
Srour Aladdin M, Ismail Abd El-Hamid A, El-Kosy Salah M, Zeid Ibrahim E
机构信息
Therapeutical Chemistry Department, National Research Centre, Cairo, Egypt.
出版信息
Z Naturforsch C J Biosci. 2009 Jul-Aug;64(7-8):483-9. doi: 10.1515/znc-2009-7-803.
The pyrimidine thione derivatives 2a-d were prepared by the reaction of thiourea, ethyl cyanoacetate and several aromatic aldehydes. The acyclic thioglycosides 4a-7d were prepared by the reaction of the synthesized pyrimidine thiones 2a-d with different alkyl halides, whereas the reaction of 2a-d with 2,3,4,6-tetra-O-acetyl-alpha-D-glucopyranosyl bromide afforded the cyclic thioglycosides 8a-d whose deprotection afforded 9a-d. The obtained compounds were tested for their antischistosomal and antiviral activity against hepatitis B virus (HBV). Compounds 5a, 5d, 7a showed high activity against HBV using the MTT assay; moreover compounds 5c, 6d, 7a, 9a, 9c exhibited high activity as antischistosomal agents.
嘧啶硫酮衍生物2a - d是通过硫脲、氰基乙酸乙酯与几种芳香醛反应制备的。无环硫代糖苷4a - 7d是由合成的嘧啶硫酮2a - d与不同的卤代烃反应制备的，而2a - d与2,3,4,6 - 四 - O - 乙酰基 - α - D - 吡喃葡萄糖基溴反应得到环状硫代糖苷8a - d，其脱保护得到9a - d。对所得化合物进行了抗血吸虫和抗乙型肝炎病毒（HBV）的抗病毒活性测试。使用MTT法，化合物5a、5d、7a对HBV表现出高活性；此外，化合物5c、6d、7a、9a、9c作为抗血吸虫剂表现出高活性。
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