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Synthesis and antiviral activity of a series of novel N-phenylbenzamide and N-phenylacetophenone compounds as anti-HCV and anti-EV71 agents
  • 时间:0
  • 分类:R914.5[医药卫生—药物化学;医药卫生—药学]
  • 作者机构:Institute of Medicinal Biotechnology,Chinese Academy of Medical Sciences and Peking Union Medical College
  • 相关基金:supported by the National Natural Science Foundation of China (Nos.81273439 and 81202414);Student Fund of Innovation Project of Peking Union Medical College (No.2013-1007-10)
中文摘要:

A series of novel N-phenylbenzamide and N-phenylacetophenone compounds were synthesized and evaluated for their antiviral activity against HCV and EV71(strain SZ-98).The biological results showed that three compounds(23,25 and 41) exhibited considerable anti-HCV activity(IC50? 0.57–7.12 μmol/L) and several compounds(23,28,29,30,31 and 42) displayed potent activity against EV71 with the IC50 values lower than 5.00 μmol/L.The potency of compound 23(IC50? 0.57 μmol/L) was superior to that of reported compounds IMB-1f(IC50? 1.90 μmol/L) and IMB-1g(IC50? 1.00 μmol/L) as anti-HCV agents,and compound29 possessed the highest anti-EV71 activity,comparable to the comparator drug pirodavir.The efficacy in vivo and antiviral mechanism of these compounds warrant further investigations.

英文摘要:

A series of novel N-phenybenzamide and N-phenylacetophenone compounds were synthesized and evaluated for their antiviral activity against HCV and EV71 (strain SZ-98). The biological results showed that three compounds (23, 25 and 41) exhibited considerable anti-HCV activity (IC50 = 0.57-7.12 mu mol/L) and several compounds 123, 28, 29, 30, 31 and 42) displayed potent activity against EV71 with the IC50 values lower than 5.00 mu mol/L. The potency of compound 23 (IC50= 0.57 mu mol/L) was superior to that of reported compounds [IMB-If (IC50 = 1.90 mu mol/L) and IMB-1 (IC50 = 1.00 mu mol/L) as anti-HCV agents, and compound 29 possessed the highest anti-EV71 activity, comparable to the comparator drug pirodavir. The efficacy in vivo and antiviral mechanism of these compounds warrant further investigations. (C) 2015 Chinese Pharmaceutical Association and Institute of Materia Medial., Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.

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