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