Synthesis of diversely substituted pyridin-2(1H)-ones and in vivo evaluation of their anti-allodynic effect on cutaneous inflammatory mechanical allodynia - Archive ouverte HAL
Article Dans Une Revue RSC Medicinal Chemistry Année : 2024

Synthesis of diversely substituted pyridin-2(1H)-ones and in vivo evaluation of their anti-allodynic effect on cutaneous inflammatory mechanical allodynia

Résumé

A series of 3,5-disubtituted pyridin-2(1H)-ones was synthesized. As part of a structure–activity relationship study performed in this series, structural modifications were based on 3-(indol-4-yl)-5-(pyridin-4-ylamino)pyridin-2(1H)-one B, which exhibited a potent anti-allodynic effect in a rat model of inflammatory pain. In this study, new compounds were assessed for their ability to inhibit cutaneous mechanical allodynia in rats by using the capsaicin pain model. Compound 36, a 2-methoxypyridine derivative, yielded the most promising outcome, demonstrating an enhanced analgesic effect.
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Dates et versions

hal-04742185 , version 1 (17-10-2024)

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Théo Frazier, Pauline Murail, Arthur Boulangé, Nazim Chalane, Francis Giraud, et al.. Synthesis of diversely substituted pyridin-2(1H)-ones and in vivo evaluation of their anti-allodynic effect on cutaneous inflammatory mechanical allodynia. RSC Medicinal Chemistry, 2024, 15 (8), pp.2900-2921. ⟨10.1039/d4md00375f⟩. ⟨hal-04742185⟩
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