title: Pyrazolopyrimidines and pyrazolotriazines with potent activity against herpesviruses.
abstract: Synthesis of several pyrazolo[1,5-c]pyrimidines, pyrazolo[1,5-a]pyrimidines and pyrazolo[1,5-a][1,3,5]triazines with potent activity against herpes simplex viruses is described. Synthetic approaches allowing for variation of the substitution pattern are outlined and resulting changes in antiviral activity are highlighted. Several compounds with in vitro antiviral activity similar or better than acyclovir are described.
authors.affiliation: Department of Medicinal Chemistry, Metabolic and Virology Center of Excellence for Drug Discovery, GlaxoSmithKline Research & Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA. ksgudmundsson@gmail.com
authors.forename: Kristjan S
authors.initials: KS
authors.lastname: Gudmundsson
authors.forename: Brian A
authors.initials: BA
authors.lastname: Johns
authors.forename: Jason
authors.initials: J
authors.lastname: Weatherhead
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D002522:Chlorocebus aethiops; D006564:Herpesviridae / Q000187:drug effects*; D006566:Herpesviridae Infections / Q000188:drug therapy; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D014709:Vero Cells
chemical_list: D000998:Antiviral Agents; D011720:Pyrazoles; D011743:Pyrimidines; D014227:Triazines; C527752:pyrazolo(1,5-a)pyrimidine