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Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives
Jiangsu Key Laboratory for High Technology of TCM Formulae Research, College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China
College of Biotechnology and Pharmaceutical Engineering, Nanjing University of Technology, Nanjing 211816, China
* Authors to whom correspondence should be addressed.
Received: 8 July 2013; in revised form: 29 July 2013 / Accepted: 7 August 2013 / Published: 20 August 2013
Abstract: 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
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MDPI and ACS Style
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.
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. International Journal of Molecular Sciences. 2013; 14(8):17193-17203.
Bao, Beihua; Meng, Zheng; Li, Nianguang; Meng, Zhengjie; Zhang, Li; Cao, Yudan; Yao, Weifeng; Shan, Mingqiu; Ding, Anwei. 2013. "Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives." Int. J. Mol. Sci. 14, no. 8: 17193-17203.