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

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Frazier, Théo | Murail, Pauline | Boulangé, Arthur | Chalane, Nazim | Giraud, Francis | Artola, Alain | Dallel, Radhouane | Anizon, Fabrice | Moreau, Pascale

Edité par CCSD ; Royal Society of Chemistry -

International audience. 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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