title: Synthesis and antiviral activities of 1,2,3-triazole functionalized thymidines: 1,3-dipolar cycloaddition for efficient regioselective diversity generation.
abstract: Efficient regioselective synthesis of nucleoside conjugates was achieved by cycloaddition reaction of azides and alkynes using sodium ascorbate/ CuSO4 system as a catalyst. These 16 novel thymidine analogues were obtained in excellent yields (75-100%), employing mild reaction conditions with a broad scope of structural modification. For the compounds tested, no specific antiviral effects could be witnessed against a broad range of viruses.
authors.affiliation: Department of Chemistry and Biochemistry, Northern Arizona University, AZ, USA.
authors.forename: Longhu
authors.initials: L
authors.lastname: Zhou
authors.forename: Adel
authors.initials: A
authors.lastname: Amer
authors.forename: Michael
authors.initials: M
authors.lastname: Korn
authors.forename: Robert
authors.initials: R
authors.lastname: Burda
authors.forename: Jan
authors.initials: J
authors.lastname: Balzarini
authors.forename: Erik
authors.initials: E
authors.lastname: De Clercq
authors.forename: Earl R
authors.initials: ER
authors.lastname: Kern
authors.forename: Paul F
authors.initials: PF
authors.lastname: Torrence
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D015195:Drug Design; D008958:Models, Molecular; D013329:Structure-Activity Relationship; D013936:Thymidine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D019380:Anti-HIV Agents; D000998:Antiviral Agents; D014230:Triazoles; D013936:Thymidine