title: The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations.
abstract: Using a combination of traditional Medicinal Chemistry/SAR analysis, crystallography, and molecular modeling, we have designed and synthesized a series of novel, highly potent NNRTIs that possess broad antiviral activity against a number of key clinical mutations.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, WP14-3, 770 Sumneytown Pike, PO Box 4, West Point, PA 19486-0004, USA. tom_tucker@merck.com
authors.forename: Thomas J
authors.initials: TJ
authors.lastname: Tucker
authors.forename: Sandeep
authors.initials: S
authors.lastname: Saggar
authors.forename: John T
authors.initials: JT
authors.lastname: Sisko
authors.forename: Robert M
authors.initials: RM
authors.lastname: Tynebor
authors.forename: Theresa M
authors.initials: TM
authors.lastname: Williams
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Felock
authors.forename: Jessica A
authors.initials: JA
authors.lastname: Flynn
authors.forename: Ming-Tain
authors.initials: MT
authors.lastname: Lai
authors.forename: Yuexia
authors.initials: Y
authors.lastname: Liang
authors.forename: Georgia
authors.initials: G
authors.lastname: McGaughey
authors.forename: Meiquing
authors.initials: M
authors.lastname: Liu
authors.forename: Mike
authors.initials: M
authors.lastname: Miller
authors.forename: Gregory
authors.initials: G
authors.lastname: Moyer
authors.forename: Vandna
authors.initials: V
authors.lastname: Munshi
authors.forename: Rebecca
authors.initials: R
authors.lastname: Perlow-Poehnelt
authors.forename: Sridhar
authors.initials: S
authors.lastname: Prasad
authors.forename: Rosa
authors.initials: R
authors.lastname: Sanchez
authors.forename: Maricel
authors.initials: M
authors.lastname: Torrent
authors.forename: Joseph P
authors.initials: JP
authors.lastname: Vacca
authors.forename: Bang-Lin
authors.initials: BL
authors.lastname: Wan
authors.forename: Youwei
authors.initials: Y
authors.lastname: Yan
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001665:Binding Sites; D018360:Crystallography, X-Ray; D015195:Drug Design; D024882:Drug Resistance, Viral; D004987:Ethers / Q000737:chemistry*; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology / Q000235:genetics; D008956:Models, Chemical; D009154:Mutation; D009705:Nucleosides / Q000737:chemistry; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects* / Q000502:physiology
chemical_list: D019380:Anti-HIV Agents; D004987:Ethers; D009705:Nucleosides; D018894:Reverse Transcriptase Inhibitors