title: Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity.
abstract: A series of novel pyrazinones designed as non-nucleoside reverse transcriptase inhibitors (NNRTIs) was synthesized and their anti-HIV structure-activity relationship (SAR) was studied.
authors.affiliation: Center for Molecular Design, Janssen Pharmaceutica, Antwerpsesteenweg 37, B-2350 Vosselaar, Belgium. jheeres@prdbe.jnj.com
authors.forename: Jan
authors.initials: J
authors.lastname: Heeres
authors.forename: Marc R
authors.initials: MR
authors.lastname: de Jonge
authors.forename: Lucien M H
authors.initials: LM
authors.lastname: Koymans
authors.forename: Frits F D
authors.initials: FF
authors.lastname: Daeyaert
authors.forename: Maarten
authors.initials: M
authors.lastname: Vinkers
authors.forename: Koen J A
authors.initials: KJ
authors.lastname: Van Aken
authors.forename: Eddy
authors.initials: E
authors.lastname: Arnold
authors.forename: Kalyan
authors.initials: K
authors.lastname: Das
authors.forename: Amuri
authors.initials: A
authors.lastname: Kilonda
authors.forename: Georges J
authors.initials: GJ
authors.lastname: Hoornaert
authors.forename: Frans
authors.initials: F
authors.lastname: Compernolle
authors.forename: Marek
authors.initials: M
authors.lastname: Cegla
authors.forename: Rasha A
authors.initials: RA
authors.lastname: Azzam
authors.forename: Koen
authors.initials: K
authors.lastname: Andries
authors.forename: Marie-Pierre
authors.initials: MP
authors.lastname: de Béthune
authors.forename: Hilde
authors.initials: H
authors.lastname: Azijn
authors.forename: Rudi
authors.initials: R
authors.lastname: Pauwels
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Lewi
authors.forename: Paul A J
authors.initials: PA
authors.lastname: Janssen
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D054303:HIV Reverse Transcriptase / Q000378:metabolism*; D015497:HIV-1 / Q000187:drug effects / Q000235:genetics; D008958:Models, Molecular; D009154:Mutation; D011719:Pyrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D011719:Pyrazines; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase