Synthesis, Table of Contents Synthesis 2024; 56(13): 2093-2099DOI: 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 Recommend Article Abstract Buy Article All articles of this category 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. Key words Key wordspyridin-2(1H)-ones - synthesis optimization - palladium catalysis - mechanical allodynia - analgesics Full Text References References 1 Treede R.-D, Rief W, Barke A, Aziz Q, Bennett MI, Benoliel R, Cohen M, Evers S, Finnerup NB, First MB, Giamberardino MA, Kaasa S, Korwisi B, Kosek E, Lavand’homme P, Nicholas M, Perrot S, Scholz J, Schug S, Smith BH, Svensson P, Vlaeyen JW. S, Wang S.-J. Pain 2019; 160: 19 2 Breivik H, Eisenberg E, O’Brien T. BMC Public Health 2013; 13: 1229 3 Fayaz A, Croft P, Langford RM, Donaldson LJ, Jones GT. BMJ Open 2016; 6: e010364 4 Dahlhamer J, Lucas J, Zelaya C, Nahin R, Mackey S, DeBar L, Kerns R, Von Korff M, Porter L, Helmick C. Morb. Mortal. Wkly. Rep. 2018; 67: 1001 5 Visseq A, Descheemaeker A, Pinto-Pardo N, Nauton L, Théry V, Giraud F, Abrunhosa-Thomas I, Artola A, Anizon F, Dallel R, Moreau P. Eur. J. Med. Chem. 2020; 187: 111917 6 Visseq A, Descheemaeker A, Hérault K, Giraud F, Abrunhosa-Thomas I, Artola A, Anizon F, Dallel R, Moreau P. Eur. J. Med. Chem. 2021; 225: 113748 7 Meyer-Eppler G, Küchler L, Tenten C, Benkhäuser C, Brück S, Lützen A. Synthesis 2014; 46: 1085 8 Castro AC, McGovern KJ, Burke M. Pat. Appl. WO2021127301, 2021 9 Singh BK, Cavalluzzo C, De Maeyer M, Debyser Z, Parmar VS, Van der Eycken E. Synthesis 2009; 2725 10 Dallel R, Descheemaeker A, Luccarini P. Cephalalgia 2018; 38: 776 11 Peirs C, Bourgois N, Artola A, Dallel R. Anesthesiology 2016; 124: 1136 Supplementary Material Supplementary Material Supporting Information
