Synthesis and Antiviral Activity of Novel Pyrazole Amides Containing α-Aminophosphonate Moiety

A series of novel pyrazole amides J(1)-J(15) containing an alpha-aminophosphonate moiety were synthesized and subsequently characterized by spectral (112, H-1-, C-13-, P-31-, and F-19-NM) data and elemental analysis. The racemic sample of J(1) was further separated into its enantiomers under normal-phase condition on two immobilized polysaccharide-based chiral stationary phases (Chiralpak IA and Chiralpak IC). The synthesized compounds revealed certain degree of antiviral activity in the bioassay. The title compounds (J(3) J(10), and J(12)) showed some curative activities (39.9%, 41.8%, 50.1%, respectively) against tobacco mosaic virus at 0.5 mg/mL.