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Antimicrobial Agents and Chemotherapy, December 2002, p. 4004-4008, Vol. 46, No. 12
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.12.4004-4008.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

Structure-Activity Relationship of a New Class of Anti-Hepatitis B Virus Agents

Anand Mehta,1* Bertha Conyers,1 D. L. J. Tyrrell,2 Kathie-Anne Walters,2 Graham A. Tipples,3 Raymond A. Dwek,4 and Timothy M. Block1

Department of Biochemistry and Molecular Pharmacology, The Jefferson Center, Jefferson Medical College, Doylestown, Pennsylvania 18901-2697,1 Departments of Medical Microbiology and Immunology, University of Alberta, Edmonton, Alberta,2 National Microbiology Laboratory, Winnipeg, Manitoba, Canada,3 Department of Biochemistry, Oxford University, Oxford, United Kingdom4

Received 19 February 2002/ Returned for modification 9 May 2002/ Accepted 27 August 2002

N-Nonyl-deoxy-galactonojirimycin (N-nonyl-DGJ) has been shown to reduce the amount of hepatitis B virus (HBV) produced by tissue cultures under conditions where cell viability is not affected. We show here that the compound N-nonyl-DGJ was effective against lamivudine-resistant HBV mutants bearing the YMDD motif in the polymerase gene, consistent with the compound's activity being distinct from those of nucleoside inhibitors. To better understand the chemical structures that influence its antiviral activity, a series of imino sugar derivatives were made and tested for their antiviral activity against HBV. This work suggests that the antiviral activity of the alkovirs requires an alkyl chain length of at least eight carbons but that the galactose-based head group can be modified with little or no loss in activity.

* Corresponding author. Mailing address: Department of Biochemistry, The Jefferson Center, Jefferson Medical College, 700 East Butler Ave., Doylestown, PA 18901. Phone: (215) 489-4905. Fax: (215) 489-4920. E-mail: anand.mehta{at}mail.tju.edu.

Antimicrobial Agents and Chemotherapy, December 2002, p. 4004-4008, Vol. 46, No. 12
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.12.4004-4008.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.



This article has been cited by other articles:

  • Stray, S. J., Bourne, C. R., Punna, S., Lewis, W. G., Finn, M. G., Zlotnick, A. (2005). A heteroaryldihydropyrimidine activates and can misdirect hepatitis B virus capsid assembly. Proc. Natl. Acad. Sci. USA 102: 8138-8143 [Abstract] [Full Text]  
  • Mehta, A. S., Gu, B., Conyers, B., Ouzounov, S., Wang, L., Moriarty, R. M., Dwek, R. A., Block, T. M. (2004). {alpha}-Galactosylceramide and Novel Synthetic Glycolipids Directly Induce the Innate Host Defense Pathway and Have Direct Activity against Hepatitis B and C Viruses. Antimicrob. Agents Chemother. 48: 2085-2090 [Abstract] [Full Text]  


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