title: Modifications of C-2 on the pyrroloquinoline template aimed at the development of potent herpesvirus antivirals with improved aqueous solubility.
abstract: A series of C-2 pyrroloquinoline analogs designed to improve aqueous solubility were examined for herpesvirus polymerase and antiviral activity. Several analogs were identified that maintained the antiviral activity of the previous development candidate against HCMV, HSV-1 and VZV, but with significantly improved aqueous solubility.
authors.affiliation: Global Research and Development, Pfizer, Inc., Kalamazoo, MI 49007, USA. jnieman@naeja.com
authors.forename: James A
authors.initials: JA
authors.lastname: Nieman
authors.forename: Sajiv K
authors.initials: SK
authors.lastname: Nair
authors.forename: Steven E
authors.initials: SE
authors.lastname: Heasley
authors.forename: Brenda L
authors.initials: BL
authors.lastname: Schultz
authors.forename: Herbert M
authors.initials: HM
authors.lastname: Zerth
authors.forename: Richard A
authors.initials: RA
authors.lastname: Nugent
authors.forename: Ke
authors.initials: K
authors.lastname: Chen
authors.forename: Kevin J
authors.initials: KJ
authors.lastname: Stephanski
authors.forename: Todd A
authors.initials: TA
authors.lastname: Hopkins
authors.forename: Mary L
authors.initials: ML
authors.lastname: Knechtel
authors.forename: Nancee L
authors.initials: NL
authors.lastname: Oien
authors.forename: Janet L
authors.initials: JL
authors.lastname: Wieber
authors.forename: Michael W
authors.initials: MW
authors.lastname: Wathen
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D003587:Cytomegalovirus / Q000187:drug effects; D004259:DNA-Directed DNA Polymerase / Q000378:metabolism; D006564:Herpesviridae / Q000201:enzymology*; D018259:Herpesvirus 1, Human / Q000187:drug effects; D014645:Herpesvirus 3, Human / Q000187:drug effects; D006801:Humans; D019384:Nucleic Acid Synthesis Inhibitors; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D012995:Solubility; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D019384:Nucleic Acid Synthesis Inhibitors; D011758:Pyrroles; D011804:Quinolines; C410406:pyrroloquinoline; D004259:DNA-Directed DNA Polymerase