Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 25, Issue 2, Pages 241-244Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.11.065
Keywords
Pyrimidofuroxan nucleoside; Vesicular stomatitis virus; Nitric oxide; Quantitative structure-activity relationship (QSAR)
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Funding
- National Natural Science Foundation of China [21102125]
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We have synthesized a series of 4H,6H-[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 compound 9 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. (C) 2014 Elsevier Ltd. All rights reserved.
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