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一些新合成的三唑并[4,3 - b]哒嗪的抗甲型肝炎病毒活性

Anti-HAV activity of some newly synthesized triazolo[4,3-b]pyridazines.

作者信息

Shamroukh Ahmed H, Ali Mohamed A

机构信息

Photochemistry Department, National Research Centre, Dokki, Cairo, Egypt.

出版信息

Arch Pharm (Weinheim). 2008 Apr;341(4):223-30. doi: 10.1002/ardp.200700181.

Abstract

6-Phenyl-[1,2,4]triazolo[4,3-b]pyridazine-3(2H)-thione 2 was used as precursor for the preparation of some novel 3-S-substituted-6-phenyl-[1,2,4]triazolo[4,3-b]pyridazine derivatives 3-11. Furthermore, the preparation of 1-[2-(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl)-acetyl]-1H-pyrazole derivative 13 and 5-(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanylmethyl)-[1,3,4]oxadiazole derivatives 15 and 17, are described. Some of the prepared products revealed a promising antiviral activity against 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 the test compounds. Compound 15 showed the highest effect on HAV compared to the other tested compounds.

摘要

6-苯基-[1,2,4]三唑并[4,3-b]哒嗪-3(2H)-硫酮2用作制备一些新型3-S-取代的6-苯基-[1,2,4]三唑并[4,3-b]哒嗪衍生物3-11的前体。此外,还描述了1-[2-(6-苯基-[1,2,4]三唑并[4,3-b]哒嗪-3-基硫烷基)-乙酰基]-1H-吡唑衍生物13和5-(6-苯基-[1,2,4]三唑并[4,3-b]哒嗪-3-基硫烷基甲基)-[1,3,4]恶二唑衍生物15和17的制备。一些制备的产物显示出对甲型肝炎病毒(HAV,MBB细胞培养适应株)有良好的抗病毒活性。采用蚀斑减少感染性试验来确定用测试化合物处理后病毒数量的减少。与其他测试化合物相比,化合物15对HAV的作用最强。

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