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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. Holy,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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