Synthesis and Quantitative Structure–activity Relationship (QSAR) Analysis of Some Novel Oxadiazolo[3, 4-d]pyrimidine Nucleosides Derivatives as Antiviral Agents PDF
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Published on 2015 by
Graphical abstract: Abstract: We have synthesized a series of 4 H, 6 H -[1, 2, 5]oxadiazolo[3, 4- d ]pyrimidine-5, 7-dione 1-oxide nucleoside and their anti-vesicular stomatitis virus (VSV) activities in Wish cell were also investigated in vitro. It was found that most compounds showed obvious anti-VSV activities and compound9 with ribofuranoside improved the anti-VSV activity by approximately 10 times and 18 times compared to didanosine (DDI) and acyclovir, respectively. A quantitative structure–activity relationship (QSAR) study of these compounds as well as previous reported oxadiazolo[3, 4- d ]pyrimidine nucleoside derivatives indicated that compounds with high activity should have small values of log P ( o / w ), vsurf_G and a large log S value. These findings and results provide a base for further investigations.
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