title: Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1.
abstract: The discovery and SAR study of a series of 4,6-diamino-1,3,5-triazin-2-ol compounds as novel HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are reported. The lead compounds in this series showed excellent activity against wild-type and drug-resistant RT enzymes and viral strains. In addition, compounds from this series demonstrated favorable pharmacokinetic profile in rat. A preliminary modeling study was conducted to understand the binding mode of this series of compounds.
authors.affiliation: Ansaris, Four Valley Square, 512 E. Township Line Rd, Blue Bell, PA 19422, United States. bliu@ansarisbio.com
authors.forename: Bin
authors.initials: B
authors.lastname: Liu
authors.forename: Younghee
authors.initials: Y
authors.lastname: Lee
authors.forename: Jinming
authors.initials: J
authors.lastname: Zou
authors.forename: H Michael
authors.initials: HM
authors.lastname: Petrassi
authors.forename: Rhoda W
authors.initials: RW
authors.lastname: Joseph
authors.forename: Wenchun
authors.initials: W
authors.lastname: Chao
authors.forename: Enrique L
authors.initials: EL
authors.lastname: Michelotti
authors.forename: Marina
authors.initials: M
authors.lastname: Bukhtiyarova
authors.forename: Eric B
authors.initials: EB
authors.lastname: Springman
authors.forename: Bruce D
authors.initials: BD
authors.lastname: Dorsey
mesh_terms: D000818:Animals; D055808:Drug Discovery; D008958:Models, Molecular; D051381:Rats; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D018894:Reverse Transcriptase Inhibitors; D014227:Triazines