Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives
Open Access
- 20 August 2013
- journal article
- research article
- Published by MDPI AG in International Journal of Molecular Sciences
- Vol. 14 (8), 17193-17203
- https://doi.org/10.3390/ijms140817193
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.This publication has 16 references indexed in Scilit:
- Qualitative and Quantitative Studies on Impurities in Schizonepetin, a Novel Antiviral Agent, Using HPLC, NMR and MSChromatographia, 2013
- Effects of Schizonepetin on Activity and mRNA Expression of Cytochrome P450 Enzymes in RatsInternational Journal of Molecular Sciences, 2012
- Pharmacokinetics and tissue distribution of schizonepetin in ratsFitoterapia, 2011
- Anti-HSV activity of camptothecin analoguesNatural Product Research, 2010
- Extracts and molecules from medicinal plants against herpes simplex virusesAntiviral Research, 2005
- Tandem Diels−Alder/Fragmentation Approach to the Synthesis of EleutherobinOrganic Letters, 2003
- Herpes Simplex VirusesClinical Infectious Diseases, 1998
- Molecular mechanisms of antiviral resistanceAntiviral Research, 1995
- Altered Sensitivity to Antiviral Drugs of Herpes Simplex Virus Isolates from a Patient with the Acquired Immunodeficiency SyndromeThe Journal of Infectious Diseases, 1990
- Identification of Patients with Increased Risk of Infection with Herpes Simplex Virus after Renal TransplantationThe Journal of Infectious Diseases, 1979