Synthesis and Radioprotective Effects of New Phosphorothioates Derived From Naphthylmethylimidazoline and Naphthylethylimidazoline

Abstract

A number of 2-(1-naphthylmethyl)-2-imidazoline, 2-[1-(1-naphthylethyl]-2-imidazoline, phosphorothioates, and related compounds were prepared for an evaluation as radioprotective agents against γ-rays. In this work, we report the synthesis and evaluation in vivo (radioprotective efficacy and toxicity) of new phosphorothioates. All these derivatives have shown a dose reduction factor between 1.5 and 1.9, which traduces their excellent radioprotective activity. These compounds should present an interest in chimio- and radiotherapy treatments.

Keywords:

• Naphthylmethylimidazoline
• naphthylethylimidazoline
• phosphorothioates
• Radioprotection
• WR-2721

Acknowledgments

The authors wish to thank the Délégation Générale pour l'Armement (DGA/DSP/ STTC/DT/SH), Ministère de la Défense Nationale, France, for their financial support and their interest in this research.