title: Evaluation of (E)-5-(2-bromovinyl)- and 5-vinyl-1-beta-D-arabinofuranosyluracil (BrVaraU, VaraU) in the treatment of experimental herpes simplex virus type 1 keratitis in rabbits: comparison with (E)-5-(2-bromovinyl)-2'-deoxyuridine (BrVUdR).
abstract: The 5-substituted 1-beta-D-arabinofuranosyl (araU) analogues, (E)-5-(2-bromovinyl)-araU (BrVaraU) and 5-vinyl-araU (VaraU), which can be considered as structural analogues of (E)-5-(2-bromovinyl)-2'-deoxyuridine (BrVUdR), are potent and selective inhibitors of herpes simplex virus type 1 (HSV-1) replication in vitro. BrVaraU and VaraU have been compared with BrVUdR for their therapeutic effect on acute HSV-1 keratitis in rabbits. Both araU derivatives applied as 0.1% eyedrops suppressed the development of keratitis as monitored by the reduced number of herpes efflorescences. The healing effect of BrVaraU and VaraU was less pronounced than that of 0.1% BrVUdR eyedrops, the difference between BrVUdR and VaraU being statistically significant at the 10th day of treatment. As a further indication of the healing effect the number of cornea with opacities seen after cessation of drug treatment were 3.3, 7.4, 27.6 and 46.9% for the BrVUdR-BrVaraU-, VaraU- and placebo-treated eyes, respectively.
authors.affiliation: Clinic of Eye Diseases, Medical Academy Erfurt, D.D.R.
authors.forename: H
authors.initials: H
authors.lastname: Töpke
authors.forename: M
authors.initials: M
authors.lastname: Gräf
authors.forename: P
authors.initials: P
authors.lastname: Wutzler
authors.forename: G
authors.initials: G
authors.lastname: Herrmann
authors.forename: J
authors.initials: J
authors.lastname: Reefschläger
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000008:administration & dosage / Q000627:therapeutic use*; D001086:Arabinofuranosyluracil / Q000031:analogs & derivatives / Q000627:therapeutic use; D001973:Bromodeoxyuridine / Q000031:analogs & derivatives / Q000627:therapeutic use; D004353:Drug Evaluation, Preclinical; D007635:Keratitis, Dendritic / Q000188:drug therapy*; D009883:Ophthalmic Solutions; D011817:Rabbits
chemical_list: D000998:Antiviral Agents; D009883:Ophthalmic Solutions; C020235:brivudine; D001086:Arabinofuranosyluracil; C048730:5-vinyl-1-arabinofuranosyluracil; C031368:sorivudine; D001973:Bromodeoxyuridine