title: Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
abstract: This paper reports the synthesis and the antiviral properties of new diarylpyrimidine (DAPY) compounds as nonnucleoside reverse transcriptase inhibitors (NNRTIs). The synthesis program around this new DAPY series was further optimized to produce compounds displaying improved activity against a panel of eight clinically relevant single and double mutant strains of human immunodeficiency virus type 1 (HIV-1).
authors.affiliation: Medicinal Chemistry Department, Johnson & Johnson Pharmaceutical Research and Development, Campus de Maigremont BP615, Val de Reuil, France. jguillem@prdfr.jnj.com
authors.forename: Jerome
authors.initials: J
authors.lastname: Guillemont
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Pasquier
authors.forename: Patrice
authors.initials: P
authors.lastname: Palandjian
authors.forename: Daniel
authors.initials: D
authors.lastname: Vernier
authors.forename: Sandrine
authors.initials: S
authors.lastname: Gaurrand
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Lewi
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 H
authors.initials: MH
authors.lastname: Vinkers
authors.forename: Eddy
authors.initials: E
authors.lastname: Arnold
authors.forename: Kalyan
authors.initials: K
authors.lastname: Das
authors.forename: Rudi
authors.initials: R
authors.lastname: Pauwels
authors.forename: Koen
authors.initials: K
authors.lastname: Andries
authors.forename: Marie-Pierre
authors.initials: MP
authors.lastname: de Béthune
authors.forename: Eva
authors.initials: E
authors.lastname: Bettens
authors.forename: Kurt
authors.initials: K
authors.lastname: Hertogs
authors.forename: Piet
authors.initials: P
authors.lastname: Wigerinck
authors.forename: Philip
authors.initials: P
authors.lastname: Timmerman
authors.forename: Paul A J
authors.initials: PA
authors.lastname: Janssen
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D002460:Cell Line; D024882:Drug Resistance, Viral; D054303:HIV Reverse Transcriptase / Q000235:genetics / Q000378:metabolism*; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D009154:Mutation; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase