title: Novel acyclic nucleoside phosphonate analogues with potent anti-hepatitis B virus activities.
abstract: 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.
authors.affiliation: Rega Institute for Medical Research, Minderbroedersstraat 10, 3000 Leuven, Belgium.
authors.forename: C
authors.initials: C
authors.lastname: Ying
authors.forename: A
authors.initials: A
authors.lastname: Holy
authors.forename: D
authors.initials: D
authors.lastname: Hocková
authors.forename: Z
authors.initials: Z
authors.lastname: Havlas
authors.forename: E
authors.initials: E
authors.lastname: De Clercq
authors.forename: J
authors.initials: J
authors.lastname: Neyts
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000494:pharmacology; D000998:Antiviral Agents / Q000494:pharmacology*; D006515:Hepatitis B virus / Q000187:drug effects*; D009705:Nucleosides / Q000494:pharmacology*; D063065:Organophosphonates / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D009705:Nucleosides; D063065:Organophosphonates; C053001:adefovir; D000225:Adenine
references.citation: J Viral Hepat. 2000 Mar;7(2):161-5
references.pmid: 10760047
references.citation: J Med Chem. 2002 Apr 25;45(9):1918-29
references.pmid: 11960502
references.citation: Antimicrob Agents Chemother. 2002 Jul;46(7):2185-93
references.pmid: 12069973
references.citation: Curr Pharm Des. 2003;9(31):2567-92
references.pmid: 14529543
references.citation: J Med Chem. 2003 Nov 6;46(23):5064-73
references.pmid: 14584956
references.citation: Antimicrob Agents Chemother. 1998 Aug;42(8):2128-31
references.pmid: 9687422
references.citation: Bioorg Med Chem Lett. 2004 Aug 16;14(16):4313-7
references.pmid: 15261293
references.citation: Antimicrob Agents Chemother. 1993 Feb;37(2):332-8
references.pmid: 8452366
references.citation: Biochem Biophys Res Commun. 1996 Feb 15;219(2):337-41
references.pmid: 8604988
references.citation: Antimicrob Agents Chemother. 1997 Aug;41(8):1715-20
references.pmid: 9257747
references.citation: Bioorg Med Chem. 2004 Jun 15;12(12):3197-202
references.pmid: 15158787