Phosphonate Derivatives of Paracetamol and Valproic Acid

Paracetamol and valproic acid are standalone drugs with leading position in the world drug market. The phosphonate analogues of these drugs were synthesized and were tested in vivo. N-(4-hydroxyphenylcarbamoyl)phosphonic acid was four times more potent than paracetamol in preventing acetic acid-induced writhing. Phosphonate derivative of valproic acid, (2-propylpentanoyl)phosphonic acid, had similar in vivo activity to valproic acid in the pentylenetetrazole-induced kindling mouse model.

Automated summary

Paracetamol and valproic acid, two leading drugs in the world drug market, were examined along with their phosphonate analogues. N-(4-hydroxyphenylcarbamoyl)phosphonic acid exhibited four times greater efficacy than paracetamol in preventing acetic acid-induced writhing. The phosphonate derivative of valproic acid, (2-propylpentanoyl)phosphonic acid, demonstrated similar in vivo activity to valproic acid in the pentylenetetrazole-induced kindling mouse model.