RESUMEN

A series of 5-substituted 2'-deoxy-4'-thiopyrimidine nucleosides was synthesized and evaluated as potential antiviral agents. A number of analogues such as 2'-deoxy-5-propyl-4'-thiouridine (3ii), 2'-deoxy-5-isopropyl-4'-thiouridine (3iii), 5-cyclopropyl-2'-deoxy-4'-thiouridine (3iv), 2'-deoxy-4'-thio-5-vinyluridine (3viii), and 5-(2-chloroethyl)-2'-deoxy-4'-thiouridine (3xx) were found to be highly active against herpes simplex virus type-1 (HSV-1) and varicella zoster virus (VZV) in vitro with no significant cytotoxicity. The compound with the broadest spectrum of activity was 2'-deoxy-5-ethyl-4'-thiouridine (3i) which showed significant activity against HSV-1, HSV-2, and VZV.

Asunto(s)

Antivirales/síntesis química , Antivirales/farmacología , Nucleósidos de Pirimidina/síntesis química , Nucleósidos de Pirimidina/farmacología , Simplexvirus/efectos de los fármacos , Animales , Línea Celular , Supervivencia Celular/efectos de los fármacos , Chlorocebus aethiops , Humanos , Células Vero , Ensayo de Placa Viral