Synthesis of C3-arylated-3-deazauridine derivatives with potent anti-HSV-1 activities

Julien Lalut; Ludovic Tripoteau; Christel Marty; Hugo Bares; Nathalie Bourgougnon; François-Xavier Felpin

doi:10.1016/j.bmcl.2012.10.047

Synthesis of C3-arylated-3-deazauridine derivatives with potent anti-HSV-1 activities

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7461-4. doi: 10.1016/j.bmcl.2012.10.047. Epub 2012 Oct 24.

Authors

Julien Lalut¹, Ludovic Tripoteau, Christel Marty, Hugo Bares, Nathalie Bourgougnon, François-Xavier Felpin

Affiliation

¹ Université Bordeaux 1, UMR CNRS 5255, Institut des Sciences Moléculaires, 351 Cours de la Libération, 33405 Talence Cedex, France.

PMID: 23141915
DOI: 10.1016/j.bmcl.2012.10.047

Abstract

A series of 3-deazauridines (3-DU) analogues were synthesized and evaluated in vitro for their antiherpetic activity against HSV-1 on Vero cell lines by cell viability. A first campaign of tests suggested that C3-arylated-3-DU derivatives could constitute a novel family of antiherpetic agents. A second campaign of biological evaluations led to the discovery of two potent anti-HSV-1 agents with comparable activity than acyclovir.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

3-Deazauridine / analogs & derivatives
3-Deazauridine / chemical synthesis
3-Deazauridine / pharmacology*
Animals
Antiviral Agents / chemical synthesis
Antiviral Agents / chemistry
Antiviral Agents / pharmacology*
Cell Survival / drug effects
Chlorocebus aethiops
Dose-Response Relationship, Drug
Herpesvirus 1, Human / drug effects*
Microbial Sensitivity Tests
Molecular Structure
Structure-Activity Relationship
Vero Cells

Substances

Antiviral Agents
3-Deazauridine