Synthesis and antiviral activity of a series of novel N-phenylbenzamide and N-phenylacetophenone compounds as anti-HCV and anti-EV71 agents

  • Acta Pharm Sin B. 2015 May;5(3):201-9. doi: 10.1016/j.apsb.2015.03.013.
Zhi Jiang  1 ,  Huiqiang Wang  1 ,  Yanping Li  1 ,  Zonggen Peng  1 ,  Yuhuan Li  1 ,  Zhuorong Li  1
Affiliations
  • 1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
PMID: 26579447 DOI: 10.1016/j.apsb.2015.03.013
Abstract

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 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.

Keywords
Agents; Anti-EV71; Anti-HCV; N-phenylacetophenone; N-phenylbenzamide; Synthesis.
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