title: Design, synthesis and antiviral activity studies of schizonepetin derivatives.
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.
authors: Jiangsu Key Laboratory for High Technology of TCM Formulae Research, College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China. beihua.bao@gmail.com
authors: Beihua
authors: B
authors: Bao
authors: Zheng
authors: Z
authors: Meng
authors: Nianguang
authors: N
authors: Li
authors: Zhengjie
authors: Z
authors: Meng
authors: Li
authors: L
authors: Zhang
authors: Yudan
authors: Y
authors: Cao
authors: Weifeng
authors: W
authors: Yao
authors: Mingqiu
authors: M
authors: Shan
authors: Anwei
authors: A
authors: Ding
mesh_terms: D000212:Acyclovir / Q000494:pharmacology; D000215:Acylation; D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D004951:Esterification; D018259:Herpesvirus 1, Human / Q000187:drug effects*; D053122:Influenza A Virus, H3N2 Subtype / Q000187:drug effects*; D020128:Inhibitory Concentration 50; D061985:Madin Darby Canine Kidney Cells; D039821:Monoterpenes / Q000138:chemical synthesis / Q000494:pharmacology*; D014709:Vero Cells
chemical_list: D000998:Antiviral Agents; D039821:Monoterpenes; C570489:schizonepetin; D000212:Acyclovir
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