Phosphonoamidates &amp; Phosphopnoamidines: A convenient Synthesis, Spectroscopic Properties, DFT Calculations &amp; Pharmacological Studies

Omrani, Rania; Ali, Ridha Ben; Arfaoui, Youssef; Raddaoui, Anis; Hmani, Hedia; May, Michèle Véronique El; Akacha, Azaiez Ben

doi:10.1016/j.molstruc.2021.130321

Cited by 4 publications

(1 citation statement)

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“…The scaffold has been examined as antimicrobials, [18] Src SH2 domain ligands, [19] anti‐tumor agents [20] and human thyroid hormone agonists [21] . A recent paper published after this work was completed revealed that N ‐(4‐chlorophenylcarbamoyl)phosphonic acid possessed weak antimicrobial activity as well as some analgesic activity in multiple animal pain models [22] . However, the exact derivative possessing the paracetamol core structure (compound 3 ) was not described.…”

Section: Discussionmentioning

confidence: 99%

Phosphonate Derivatives of Paracetamol and Valproic Acid

et al. 2022

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Dedicated to Prof György Keglevich on the occasion of his 65 th birthday.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, (2propylpentanoyl)phosphonic acid, had similar in vivo activity to valproic acid in the pentylenetetrazole-induced kindling mouse model.

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