Synthesis and SAR Studies of Isoquinoline and Tetrahydroisoquinoline Derivatives as Melatonin Receptor Ligands

Autor: Maxime Liberelle, Philippe Delagrange, Amélie Laversin, Daniel Henri Caignard, Nicolas Lebegue, Mohamed Ettaoussi, Saïd Yous, Marouane Rami, Patricia Melnyk, Brandon Vreulz

Publikováno v: ChemMedChem. 17(3)

In our constant search for new successors of agomelatine, we report herein a new series of compounds resulting from bioisosteric modulation of the naphthalene ring. The isoquinoline and tetrahydroisoquinoline derivatives were synthesized and pharmaco

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f47969380e40559daea3163ab647855
https://pubmed.ncbi.nlm.nih.gov/34797951

Discovery of holoenzyme-disrupting chemicals as substrate-selective CK2 inhibitors

Autor: Ruben Abagyan, Renaud Prudent, Thierry Lomberget, Céline F. Sautel, Béatrice Laudet, Matthias Engel, Isabelle Krimm, Odile Filhol, Marc Le Borgne, Irina Kufareva, Mohamed Ettaoussi, Claude Cochet, Paul Brear, Benoit Bestgen, Virginie Moucadel

Publikováno v: Scientific Reports
Scientific Reports, Nature Publishing Group, 2019, 9 (1), ⟨10.1038/s41598-019-52141-5⟩
Scientific Reports, Nature Publishing Group, 2019, 9 (1), pp.15893. ⟨10.1038/s41598-019-52141-5⟩
Scientific Reports, 2019, 9 (1), pp.15893. ⟨10.1038/s41598-019-52141-5⟩
Scientific reports, vol 9, iss 1
Scientific Reports, Vol 9, Iss 1, Pp 1-16 (2019)

CK2 is a constitutively active protein kinase overexpressed in numerous malignancies. Interaction between CK2α and CK2β subunits is essential for substrate selectivity. The CK2α/CK2β interface has been previously targeted by peptides to achieve f

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb42963b4bb31b7a9a23b98e865c8e28
https://hal.archives-ouvertes.fr/hal-02466039

Melatonin MT 1 receptor as a novel target in neuropsychopharmacology: MT 1 ligands, pathophysiological and therapeutic implications, and perspectives

Autor: Fabrizia C. Guarnieri, Stefano Comai, Danilo De Gregorio, Mohamed Ettaoussi, Martha Lopez-Canul, Ada R. Posner, Gabriella Gobbi

Melatonin (MLT), a neuromodulator mainly acting through two G-protein coupled receptors MT 1 and MT 2 , regulates many brain functions, including circadian rhythms, mood, pain and sleep. MLT and non-selective MT 1 /MT 2 receptor agonists are clinical

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b3f96cb3e81f92412f806a1298042e1
http://www.elsevier.com/inca/publications/store/6/2/2/9/3/1/index.htt

Synthesis and pharmacological evaluation of dual ligands for melatonin (MT1/MT2) and serotonin 5-HT2C receptor subtypes (II)

Autor: Patricia Melnyk, Pascal Berthelot, Basile Pérès, Jean A. Boutin, Philippe Delagrange, Saïd Yous, Aïcha Errazani, Daniel-Henri Caignard, Mohamed Ettaoussi

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2015, 90, pp.822-833. ⟨10.1016/j.ejmech.2014.12.021⟩
European Journal of Medicinal Chemistry, 2015, 90, pp.822-833. ⟨10.1016/j.ejmech.2014.12.021⟩

International audience; In this paper we report the investigation of C-3 and β-acetamide positions of agomelatine analogues. Concomitant insertion of a hydroxymethyl in the β-acetamide position and aliphatic groups in C-3 position produced a positi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d0f126b044ca9622cbac66b3989475aa
https://doi.org/10.1016/j.ejmech.2014.12.021

New quinolinic derivatives as melatonergic ligands: Synthesis and pharmacological evaluation

Autor: Elodie Landagaray, Daniel-Henri Caignard, Pascal Berthelot, Patricia Melnyk, Marouan Rami, Saïd Yous, Jean A. Boutin, Mohamed Ettaoussi, Philippe Delagrange

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2017, 127, pp.621-631. ⟨10.1016/j.ejmech.2016.12.013⟩
European Journal of Medicinal Chemistry, 2017, 127, pp.621-631. ⟨10.1016/j.ejmech.2016.12.013⟩

New series of melatonergic ligands issued from two methoxy-quinolinic scaffolds (2-MQ and 3-MQ), were designed and synthesized. Herein we report the synthetic scheme and pharmacological results of the new prepared compounds. Investigation of compound

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eff324fee630435dee54dfde56bcd365
https://hal.archives-ouvertes.fr/hal-02060568