Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.
A series of 4,4-disubstituted quinolinones was prepared and evaluated as HIV-1 reverse transcriptase inhibitors. The C-3 substituted compound 9h displayed improved antiviral activity against clinically significant single (K103N) and double (K103N/L100I) mutant viruses.
Patel
M
M
DuPont Pharmaceuticals Company, Experimental Station, E500/4803, PO Box 80500, 19880-0500, Wilmington, DE, USA. mpatel5@prius.jnj.com
McHugh
R J
RJ
Cordova
B C
BC
Klabe
R M
RM
Bacheler
L T
LT
Erickson-Viitanen
S
S
Rodgers
J D
JD
D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D004351:Drug Resistance / Q000235:genetics; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D020128:Inhibitory Concentration 50; D009154:Mutation / Q000235:genetics; D015363:Quinolones / Q000138:chemical synthesis / Q000494:pharmacology*
D000998:Antiviral Agents; D015363:Quinolones; D054303:HIV Reverse Transcriptase