title: Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
abstract: The synthesis and anti-HIV-1 activity of a series of diarylpyrimidines (DAPYs) are described. Several members of this novel class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) are extremely potent against both wild-type and a panel of clinically significant single- and double-mutant strains of HIV-1.
authors.affiliation: Janssen Research Foundation, Welsh and McKean Roads, Spring House, PA 19477, USA.
authors.forename: D W
authors.initials: DW
authors.lastname: Ludovici
authors.forename: B L
authors.initials: BL
authors.lastname: De Corte
authors.forename: M J
authors.initials: MJ
authors.lastname: Kukla
authors.forename: H
authors.initials: H
authors.lastname: Ye
authors.forename: C Y
authors.initials: CY
authors.lastname: Ho
authors.forename: M A
authors.initials: MA
authors.lastname: Lichtenstein
authors.forename: R W
authors.initials: RW
authors.lastname: Kavash
authors.forename: K
authors.initials: K
authors.lastname: Andries
authors.forename: M P
authors.initials: MP
authors.lastname: de Béthune
authors.forename: H
authors.initials: H
authors.lastname: Azijn
authors.forename: R
authors.initials: R
authors.lastname: Pauwels
authors.forename: P J
authors.initials: PJ
authors.lastname: Lewi
authors.forename: J
authors.initials: J
authors.lastname: Heeres
authors.forename: L M
authors.initials: LM
authors.lastname: Koymans
authors.forename: M R
authors.initials: MR
authors.lastname: de Jonge
authors.forename: K J
authors.initials: KJ
authors.lastname: Van Aken
authors.forename: F F
authors.initials: FF
authors.lastname: Daeyaert
authors.forename: K
authors.initials: K
authors.lastname: Das
authors.forename: E
authors.initials: E
authors.lastname: Arnold
authors.forename: P A
authors.initials: PA
authors.lastname: Janssen
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry* / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors / Q000187:drug effects / Q000235:genetics; D015497:HIV-1 / Q000187:drug effects / Q000235:genetics; D020128:Inhibitory Concentration 50; D009154:Mutation; D009570:Nitriles / Q000737:chemistry* / Q000494:pharmacology*; D011743:Pyrimidines / Q000737:chemistry* / Q000494:pharmacology*; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: C442363:6-amino-5-bromo-4-(4-cyano-2,6-dimethylphenoxy)-2-(4-cyanophenylamino)pyrimidine; D019380:Anti-HIV Agents; D009570:Nitriles; D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase