Pyridin-2(1H)one derivatives: A possible new class of therapeutics for mechanical allodynia

Visseq, A.; Descheemaeker, Amélie; Pinto-Pardo, Nicolás; Nauton, Lionel; Théry, Vincent; Giraud, F; Abrunhosa-Thomas, Isabelle; Artola, Alain; Anizon, Fabrice; Dallel, Radhouane; Moreau, Pascale

doi:10.1016/j.ejmech.2019.111917

Cited by 8 publications

(14 citation statements)

References 28 publications

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“…Finally, compound 12 is a pyridinone derivative recently reported as a selective p38α MAPK inhibitor, with an IC 50 value of 1.5 µM ( Figure 12 ) [ 50 ]. Its selectivity was demonstrated using a panel of 62 protein kinases including p38 isoforms and protein kinases close to p38 in the phylogenetic tree.…”

Section: Cmgc Groupmentioning

confidence: 99%

Recent Advances in Pain Management: Relevant Protein Kinases and Their Inhibitors

et al. 2021

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The purpose of this review is to underline the protein kinases that have been established, either in fundamental approach or clinical trials, as potential biological targets in pain management. Protein kinases are presented according to their group in the human kinome: TK (Trk, RET, EGFR, JAK, VEGFR, SFK, BCR–Abl), CMGC (p38 MAPK, MEK, ERK, JNK, ASK1, CDK, CLK2, DYRK1A, GSK3, CK2), AGC (PKA, PKB, PKC, PKMζ, PKG, ROCK), CAMK, CK1 and atypical/other protein kinases (IKK, mTOR). Examples of small molecule inhibitors of these biological targets, demonstrating an analgesic effect, are described. Altogether, this review demonstrates the fundamental role that protein kinase inhibitors could play in the development of new pain treatments.

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Section: Cmgc Groupmentioning

confidence: 99%

Recent Advances in Pain Management: Relevant Protein Kinases and Their Inhibitors

et al. 2021

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“…For example, targeting p38 [9,10] suppresses spontaneous pain behavior (formalin test). Inhibition of ERK [11], PKCγ [12][13][14][15], and p38 [16][17][18] prevents inflammatory mechanical allodynia (MA). Application of p38 inhibitors [18][19][20][21] can also reduce neuropathic MA.…”

Section: Introductionmentioning

confidence: 99%

“…Inhibition of ERK [11], PKCγ [12][13][14][15], and p38 [16][17][18] prevents inflammatory mechanical allodynia (MA). Application of p38 inhibitors [18][19][20][21] can also reduce neuropathic MA. Thus, protein kinases appear to be relevant biological targets for developing new analgesics.…”

Section: Introductionmentioning

confidence: 99%

“…As part of our ongoing program dedicated to the design and synthesis of small molecules with potent protein kinase inhibitory activities and analgesic properties, we previously reported the identification of a new 3,5-disubstituted pyridin-2(1H)-one series with potent in vivo activity in rat models of inflammatory and neuropathic MA [18]. The best anti-allodynic agent of the series (compound 2, Fig.…”

Section: Introductionmentioning

confidence: 99%

“…B. Kinase selectivity of compound 2. Residual activity at 10 µM: Blue disks ≥ 65%, red disk: 19% [18]. The tree was generated using the Kinome Render software, and the illustration reproduced courtesy of Cell Signaling Technology, Inc. (www.cellsignal.com) [22].…”

Section: Introductionmentioning

confidence: 99%

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Improved potency of pyridin-2(1H)one derivatives for the treatment of mechanical allodynia

Visseq

Descheemaeker

Hérault

et al. 2021

European Journal of Medicinal Chemistry

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Synthesis of new 2‐pyridinone and thiazole derivatives containing coumarin moiety

Al‐Harbi,

Emam,

Abbas

2023

Journal of Heterocyclic Chem

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Coumarin has shown considerable therapeutic potency because of its versatile biological prosperities. Also, pyridines have been adopted in medicinal chemistry as potent ring. Moreover, several investigations reported the potency of thiazole‐containing compounds. So, during this research, new functionalized 2‐pyridinone and thiazole derivatives bearing coumarin moiety were aimed to synthesize. Many trials to obtain the 6‐amino‐2‐oxo‐pyridine‐3,5‐dicarbonitriles through the condensation of cyanoacetohydrazone of 3‐acetyl coumarin with 2‐(arylidene)malononitriles were carried out using different reaction conditions. In all cases, the reaction gave none of the corresponding 2‐pyridinone derivatives except the reaction with 2‐(benzylidene)‐malononitrile afforded product in few yield. Moreover, the reaction of another cyanoacetanilide with the 2‐(arylidene)‐malononitrile afforded the unexpected arylidene derivatives rather than the expected pyridin‐2‐one derivatives. Finally, new thiazoles bearing coumarin moiety were synthesized using 3‐acetylcoumarin N‐(2,4‐dimethoxyphenyl)‐thiosemicarbazone. Cyclization of thiosemicarbazone derivative with ethyl 2‐chloroacetate, chloroacetone or phenacyl bromide afforded in high yields the corresponding derivatives of thiazolidin‐4‐one, 4‐methylthiazole or 4‐phenylthiazole, respectively.

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Pyridin-2(1H)one derivatives: A possible new class of therapeutics for mechanical allodynia

Cited by 8 publications

References 28 publications

Recent Advances in Pain Management: Relevant Protein Kinases and Their Inhibitors

Recent Advances in Pain Management: Relevant Protein Kinases and Their Inhibitors

Improved potency of pyridin-2(1H)one derivatives for the treatment of mechanical allodynia

Synthesis of new 2‐pyridinone and thiazole derivatives containing coumarin moiety

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