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Antimicrobial Agents and Chemotherapy, March 2005, p. 1177-1180, Vol. 49, No. 3
0066-4804/05/$08.00+0 doi:10.1128/AAC.49.3.1177-1180.2005
Copyright © 2005, American Society for Microbiology. All Rights Reserved.
Novel Acyclic Nucleoside Phosphonate Analogues with Potent Anti-Hepatitis B Virus Activities
C. Ying,1
A. Hol
,2
D. Hocková,2
Z. Havlas,2
E. De Clercq,1 and
J. Neyts1*
Rega Institute for Medical Research, Leuven, Belgium,1
Institute of Organic Chemistry and Biochemistry, Academy of Sciences, Prague, Czech Republic2
Received 16 April 2004/
Returned for modification 28 May 2004/
Accepted 12 November 2004
Novel acyclic nucleoside phosphonates with a pyrimidine base preferentially containing an amino group at C-2 and C-4 and a 2-(phosphonomethoxy)ethoxy or (R)-2-(phosphonomethoxy)propoxy group at C-6 selectively inhibit the replication of wild-type and lamivudine-resistant hepatitis B viruses. The activity of the most potent compounds was comparable to that of adefovir.
* Corresponding author. Mailing address: Rega Institute, Minderbroedersstraat 10, 3000 Leuven, Belgium. Phone: 00-32-16-33.73.53. Fax: 00-32-16-33.73.40. E-mail:
Johan.Neyts{at}rega.kuleuven.ac.be.
Antimicrobial Agents and Chemotherapy, March 2005, p. 1177-1180, Vol. 49, No. 3
0066-4804/05/$08.00+0 doi:10.1128/AAC.49.3.1177-1180.2005
Copyright © 2005, American Society for Microbiology. All Rights Reserved.
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