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Superiority of the Triple-Acting 5-HT6R/5-HT3R Antagonist and MAO-B Reversible Inhibitor PZ-1922 over 5-HT6R Antagonist Intepirdine in Alleviation of Cognitive Deficits in Rats.
Grychowska K, López-Sánchez U, Vitalis M, Canet G, Satała G, Olejarz-Maciej A, Gołębiowska J, Kurczab R, Pietruś W, Kubacka M, Moreau C, Walczak M, Blicharz-Futera K, Bento O, Bantreil X, Subra G, Bojarski AJ, Lamaty F, Becamel C, Zussy C, Chaumont-Dubel S, Popik P, Nury H, Marin P, Givalois L, Zajdel P. Grychowska K, et al. Among authors: chaumont dubel s. J Med Chem. 2023 Nov 9;66(21):14928-14947. doi: 10.1021/acs.jmedchem.3c01482. Epub 2023 Oct 5. J Med Chem. 2023. PMID: 37797083 Free PMC article.
A dual-acting 5-HT6 receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties.
Canale V, Grychowska K, Kurczab R, Ryng M, Keeri AR, Satała G, Olejarz-Maciej A, Koczurkiewicz P, Drop M, Blicharz K, Piska K, Pękala E, Janiszewska P, Krawczyk M, Walczak M, Chaumont-Dubel S, Bojarski AJ, Marin P, Popik P, Zajdel P. Canale V, et al. Eur J Med Chem. 2020 Dec 15;208:112765. doi: 10.1016/j.ejmech.2020.112765. Epub 2020 Aug 22. Eur J Med Chem. 2020. PMID: 32949963
Imidazopyridine-Based 5-HT6 Receptor Neutral Antagonists: Impact of N1-Benzyl and N1-Phenylsulfonyl Fragments on Different Receptor Conformational States.
Vanda D, Canale V, Chaumont-Dubel S, Kurczab R, Satała G, Koczurkiewicz-Adamczyk P, Krawczyk M, Pietruś W, Blicharz K, Pękala E, Bojarski AJ, Popik P, Marin P, Soural M, Zajdel P. Vanda D, et al. J Med Chem. 2021 Jan 28;64(2):1180-1196. doi: 10.1021/acs.jmedchem.0c02009. Epub 2021 Jan 13. J Med Chem. 2021. PMID: 33439019
Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT3 and 5-HT6 Receptor Antagonist with Antipsychotic and Procognitive Properties.
Zajdel P, Grychowska K, Mogilski S, Kurczab R, Satała G, Bugno R, Kos T, Gołębiowska J, Malikowska-Racia N, Nikiforuk A, Chaumont-Dubel S, Bantreil X, Pawłowski M, Martinez J, Subra G, Lamaty F, Marin P, Bojarski AJ, Popik P. Zajdel P, et al. Among authors: chaumont dubel s. J Med Chem. 2021 Sep 23;64(18):13279-13298. doi: 10.1021/acs.jmedchem.1c00224. Epub 2021 Sep 1. J Med Chem. 2021. PMID: 34467765 Free PMC article.
Novel 1H-Pyrrolo[3,2-c]quinoline Based 5-HT6 Receptor Antagonists with Potential Application for the Treatment of Cognitive Disorders Associated with Alzheimer's Disease.
Grychowska K, Satała G, Kos T, Partyka A, Colacino E, Chaumont-Dubel S, Bantreil X, Wesołowska A, Pawłowski M, Martinez J, Marin P, Subra G, Bojarski AJ, Lamaty F, Popik P, Zajdel P. Grychowska K, et al. ACS Chem Neurosci. 2016 Jul 20;7(7):972-83. doi: 10.1021/acschemneuro.6b00090. Epub 2016 May 5. ACS Chem Neurosci. 2016. PMID: 27100049
Dual 5-HT6 and D3 Receptor Antagonists in a Group of 1H-Pyrrolo[3,2-c]quinolines with Neuroprotective and Procognitive Activity.
Grychowska K, Chaumont-Dubel S, Kurczab R, Koczurkiewicz P, Deville C, Krawczyk M, Pietruś W, Satała G, Buda S, Piska K, Drop M, Bantreil X, Lamaty F, Pękala E, Bojarski AJ, Popik P, Marin P, Zajdel P. Grychowska K, et al. ACS Chem Neurosci. 2019 Jul 17;10(7):3183-3196. doi: 10.1021/acschemneuro.8b00618. Epub 2019 Apr 2. ACS Chem Neurosci. 2019. PMID: 30896921
2-Phenyl-1H-pyrrole-3-carboxamide as a New Scaffold for Developing 5-HT6 Receptor Inverse Agonists with Cognition-Enhancing Activity.
Drop M, Canale V, Chaumont-Dubel S, Kurczab R, Satała G, Bantreil X, Walczak M, Koczurkiewicz-Adamczyk P, Latacz G, Gwizdak A, Krawczyk M, Gołębiowska J, Grychowska K, Bojarski AJ, Nikiforuk A, Subra G, Martinez J, Pawłowski M, Popik P, Marin P, Lamaty F, Zajdel P. Drop M, et al. ACS Chem Neurosci. 2021 Apr 7;12(7):1228-1240. doi: 10.1021/acschemneuro.1c00061. Epub 2021 Mar 11. ACS Chem Neurosci. 2021. PMID: 33705101 Free PMC article.
Neuropathic pain-alleviating activity of novel 5-HT6 receptor inverse agonists derived from 2-aryl-1H-pyrrole-3-carboxamide.
Drop M, Jacquot F, Canale V, Chaumont-Dubel S, Walczak M, Satała G, Nosalska K, Mahoro GU, Słoczyńska K, Piska K, Lamoine S, Pękala E, Masurier N, Bojarski AJ, Pawłowski M, Martinez J, Subra G, Bantreil X, Lamaty F, Eschalier A, Marin P, Courteix C, Zajdel P. Drop M, et al. Among authors: chaumont dubel s. Bioorg Chem. 2021 Oct;115:105218. doi: 10.1016/j.bioorg.2021.105218. Epub 2021 Jul 29. Bioorg Chem. 2021. PMID: 34365058 Free article.
1-(Arylsulfonyl-isoindol-2-yl)piperazines as 5-HT6R Antagonists: Mechanochemical Synthesis, In Vitro Pharmacological Properties and Glioprotective Activity.
Canale V, Trybała W, Chaumont-Dubel S, Koczurkiewicz-Adamczyk P, Satała G, Bento O, Blicharz-Futera K, Bantreil X, Pękala E, Bojarski AJ, Lamaty F, Marin P, Zajdel P. Canale V, et al. Among authors: chaumont dubel s. Biomolecules. 2022 Dec 21;13(1):12. doi: 10.3390/biom13010012. Biomolecules. 2022. PMID: 36671397 Free PMC article.
31 results