Synthesis 2024; 56(13): 2093-2099
DOI: 10.1055/s-0043-1763758
paper

Improved Synthesis and Preparation of Analogues of a Pain-Relieving Pyridin-2(1H)-one

Théo Frazier
a   Université Clermont Auvergne, CNRS, Clermont Auvergne INP, ICCF, 63000 Clermont-Ferrand, France
,
Pauline Murail
b   Université Clermont Auvergne, CHU Clermont-Ferrand, Inserm, Neuro-Dol, 63000 Clermont-Ferrand, France
,
Francis Giraud
a   Université Clermont Auvergne, CNRS, Clermont Auvergne INP, ICCF, 63000 Clermont-Ferrand, France
,
Alain Artola
b   Université Clermont Auvergne, CHU Clermont-Ferrand, Inserm, Neuro-Dol, 63000 Clermont-Ferrand, France
,
Radhouane Dallel
b   Université Clermont Auvergne, CHU Clermont-Ferrand, Inserm, Neuro-Dol, 63000 Clermont-Ferrand, France
,
Fabrice Anizon
a   Université Clermont Auvergne, CNRS, Clermont Auvergne INP, ICCF, 63000 Clermont-Ferrand, France
,
Pascale Moreau
a   Université Clermont Auvergne, CNRS, Clermont Auvergne INP, ICCF, 63000 Clermont-Ferrand, France
› Author Affiliations
This research was financed by the French Government IDEX-ISITE Initiative 16-IDEX-0001 (CAP 20-25), Université Clermont-Auvergne, Institut National de la Santé et de la Recherche Médicale (Inserm), Centre National de la Recherche Scientifique (CNRS), and the Région Auvergne-Rhône-Alpes (Pack Ambition Recherche). The authors also thank WeylChem InnoTec (Frankfurt, Germany) for financial support.


Abstract

An optimization of the synthesis of 3,5-disubstituted pyridin-2(1H)-ones with in vivo anti-allodynic activity was conducted. The optimized synthesis was employed to prepare novel analogues which were then assessed for their efficacy in preventing cutaneous mechanical allodynia in a male rat hindpaw capsaicin model.

Supporting Information



Publication History

Received: 17 April 2024

Accepted after revision: 02 May 2024

Article published online:
22 May 2024

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