Successful kinase bypass with new acyclovir phosphoramidate prodrugs

  • Bioorg Med Chem Lett. 2008 Aug 1;18(15):4364-7. doi: 10.1016/j.bmcl.2008.06.069.
Christopher McGuigan  1 ,  Marco Derudas ,  Joachim J Bugert ,  Graciela Andrei ,  Robert Snoeck ,  Jan Balzarini
Affiliations
  • 1. Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff CF10 3NB, UK. [email protected]
PMID: 18614365 DOI: 10.1016/j.bmcl.2008.06.069
Abstract

Novel phosphoramidates of acyclovir have been prepared and evaluated in vitro against acyclovir-sensitive and -resistant herpes simplex virus (HSV) types 1 and 2 and varicella-zoster virus (VZV). Unlike the parent nucleoside these novel phosphate prodrugs retain Antiviral potency versus the ACV-resistant virus strain, suggesting an efficient bypass of the viral thymidine kinase.