期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 21, 页码 5182-5186出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.09.071
关键词
Quinolinone; Vaccinia; Adenovirus; Click chemistry; High-throughput screening
资金
- National Natural Science Foundation of China (NSFC) [81273354, 81573347]
- Key Project of NSFC for International Cooperation [81420108027]
- Young Scholars Program of Shandong University (YSPSDU) [2016WLJH32]
- Science and Technology Development Project of Shandong Province [2014GSF118175, 2014GSF118012]
- Major Project of Science and Technology of Shandong Province [2015ZDJS04001]
A series of 1,2,3-triazolyl 3-hydroxy-quinazoline-2,4(1H,3H)-diones was constructed utilizing Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC) method. The biological significance of the novel synthesized quinazolines was highlighted by evaluating them in vitro for antiviral activity, wherein several compounds exhibited excellent activity specifically against vaccinia and adenovirus. Especially, 24b11 displayed the most potent inhibitory activity against vaccinia with an EC50 value of 1.7 mu M, which was 15 fold than that of the reference drug Cidofovir (EC50 = 25 mu.M). 24b13 was the most potent compound against adenovirus-2 with an EC50 value of 6.2 mu M, which proved lower than all the reference drugs. Preliminary structure-activity relationships were also discussed. To the best of our knowledge, no data are present in the literature on antiviral activity of 3-hydroxy-quinazoline-2,4(1H,3H)-diones against DNA-viruses. Thus, these findings warrant further investigations (library expansion and compound refinement) on this novel class of antiviral agents. (C) 2016 Elsevier Ltd. All rights reserved.
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