title: Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.
abstract: 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.
authors.affiliation: DuPont Pharmaceuticals Company, Experimental Station, E500/4803, PO Box 80500, 19880-0500, Wilmington, DE, USA. mpatel5@prius.jnj.com
authors.forename: M
authors.initials: M
authors.lastname: Patel
authors.forename: R J
authors.initials: RJ
authors.lastname: McHugh
authors.forename: B C
authors.initials: BC
authors.lastname: Cordova
authors.forename: R M
authors.initials: RM
authors.lastname: Klabe
authors.forename: L T
authors.initials: LT
authors.lastname: Bacheler
authors.forename: S
authors.initials: S
authors.lastname: Erickson-Viitanen
authors.forename: J D
authors.initials: JD
authors.lastname: Rodgers
mesh_terms: 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*
chemical_list: D000998:Antiviral Agents; D015363:Quinolones; D054303:HIV Reverse Transcriptase