Synthesis and Antiviral Activities of α-Aminophosphonate Derivatives Containing a Pyridazine Moiety

Abstract

The title compounds (4) were obtained by the reaction of 2-phenyl-4-chloro-5-(4-amin ophenyl)pyridazin-3(2H)-one, aldehydes, and O,O′-dialkyl phosphite under reflux conditions using dry toluene as a solvent. The preliminary bioassays indicate that the synthesized compounds have moderate to good against tobacco mosaic virus (TMV) activity. It was found that compound 4b had a good inactivation effect in vivo against TMV, with an inhibition rate of 81.0%.

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GRAPHICAL ABSTRACT

Keywords:

• α-Aminophosphonate derivatives
• antiviral activity
• pyridazine moiety
• synthesis

Acknowledgments

We are grateful for the generous financial support received from the National Key Program for Basic Research (No. 2010CB126105) and the National Natural Science Foundation of China (No 20872002).