title: Novel benzthiodiazepinones as antiherpetic agents: SAR improvement of therapeutic index by alterations of the seven-membered ring.
abstract: A series of novel benzthiodiazepinones was studied as antiherpetic agents. Significant improvements in potency and therapeutic index in a viral replication assay were realized over the starting molecule. The role of stereospecific substitution on the diazepine ring and optimal nitrogen substitution were investigated.
authors.affiliation: Department of Chemistry, Pfizer Global R&D, Ann Arbor, MI 48118, USA. harriet.hamilton@pfizer.com
authors.forename: Harriet W
authors.initials: HW
authors.lastname: Hamilton
authors.forename: Gisele
authors.initials: G
authors.lastname: Nishiguchi
authors.forename: Susan E
authors.initials: SE
authors.lastname: Hagen
authors.forename: John D
authors.initials: JD
authors.lastname: Domagala
authors.forename: Peter C
authors.initials: PC
authors.lastname: Weber
authors.forename: Stephen
authors.initials: S
authors.lastname: Gracheck
authors.forename: Stefanie L
authors.initials: SL
authors.lastname: Boulware
authors.forename: Eric C
authors.initials: EC
authors.lastname: Nordby
authors.forename: Hidetsura
authors.initials: H
authors.lastname: Cho
authors.forename: Takeshi
authors.initials: T
authors.lastname: Nakamura
authors.forename: Satoru
authors.initials: S
authors.lastname: Ikeda
authors.forename: Wataru
authors.initials: W
authors.lastname: Watanabe
mesh_terms: D000478:Alkylation; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001381:Azepines / Q000138:chemical synthesis* / Q000494:pharmacology*; D018259:Herpesvirus 1, Human / Q000187:drug effects* / Q000235:genetics; D007202:Indicators and Reagents; D007763:Lac Operon / Q000187:drug effects; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000494:pharmacology; D014779:Virus Replication / Q000187:drug effects
chemical_list: D000998:Antiviral Agents; D001381:Azepines; D007202:Indicators and Reagents; C435483:PD 146626; D013876:Thiophenes