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Int. J. Mol. Sci. 2013, 14(8), 17193-17203; doi:10.3390/ijms140817193

Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives

1,* , 1
1 Jiangsu Key Laboratory for High Technology of TCM Formulae Research, College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China 2 College of Biotechnology and Pharmaceutical Engineering, Nanjing University of Technology, Nanjing 211816, China
* Authors to whom correspondence should be addressed.
Received: 8 July 2013 / Revised: 29 July 2013 / Accepted: 7 August 2013 / Published: 20 August 2013
(This article belongs to the Section Biochemistry, Molecular Biology and Biophysics)
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A series of schizonepetin derivatives have been designed and synthesized in order to obtain potent antivirus agents. The antiviral activity against HSV-1 and influenza virus H3N2 as well as the cytotoxicity of these derivatives was evaluated by using cytopathic effect (CPE) inhibition assay in vitro. Compounds M2, M4, M5 and M34 showed higher inhibitory activity against HSV-1 virus with the TC50 values being in micromole. Compounds M28, M33, and M35 showed higher inhibitory activity against influenza virus H3N2 with their TC50 values being 96.4, 71.0 and 75.4 μM, respectively. Preliminary biological activity evaluation indicated that the anti-H3N2 and anti-HSV-1 activities improved obviously through the introduction of halogen into the structure of schizonepetin.
Keywords: chizonepetin; anti-virus activity; HSV-1; H3N2 chizonepetin; anti-virus activity; HSV-1; H3N2
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Bao, B.; Meng, Z.; Li, N.; Meng, Z.; Zhang, L.; Cao, Y.; Yao, W.; Shan, M.; Ding, A. Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives. Int. J. Mol. Sci. 2013, 14, 17193-17203.

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