title: Biaryl acids: novel non-nucleoside inhibitors of HIV reverse transcriptase types 1 and 2.
abstract: A series of biaryl acids has been found to show micromolar inhibition of the HIV reverse transcriptase (RT) from types 1 and 2 with IC50S in the micromolar range. The series was discovered by consideration of the polymerase active site and sub-structure searching of the company compound collection. Synthesis of analogues to investigate the SAR is described. Two of these compounds have shown inhibition of HIV-2 RT only.
authors.affiliation: Department of Chemistry, GlaxoWellcome Medicines Research Center, Stevenage, Oxford.
authors.forename: J
authors.initials: J
authors.lastname: Milton
authors.forename: M J
authors.initials: MJ
authors.lastname: Slater
authors.forename: A J
authors.initials: AJ
authors.lastname: Bird
authors.forename: D
authors.initials: D
authors.lastname: Spinks
authors.forename: G
authors.initials: G
authors.lastname: Scott
authors.forename: C E
authors.initials: CE
authors.lastname: Price
authors.forename: S
authors.initials: S
authors.lastname: Downing
authors.forename: D V
authors.initials: DV
authors.lastname: Green
authors.forename: S
authors.initials: S
authors.lastname: Madar
authors.forename: R
authors.initials: R
authors.lastname: Bethell
authors.forename: D K
authors.initials: DK
authors.lastname: Stammers
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D006841:Hydrocarbons, Aromatic / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D012194:RNA-Directed DNA Polymerase / Q000187:drug effects*; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D002264:Carboxylic Acids; D006841:Hydrocarbons, Aromatic; D018894:Reverse Transcriptase Inhibitors; C072416:reverse transcriptase, Human immunodeficiency virus 2; D054303:HIV Reverse Transcriptase; D012194:RNA-Directed DNA Polymerase