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Page 1
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. 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. Among authors: grychowska k. 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
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: grychowska k. 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.
Overcoming undesirable hERG affinity by incorporating fluorine atoms: A case of MAO-B inhibitors derived from 1 H-pyrrolo-[3,2-c]quinolines.
Grychowska K, Olejarz-Maciej A, Blicharz K, Pietruś W, Karcz T, Kurczab R, Koczurkiewicz P, Doroz-Płonka A, Latacz G, Keeri AR, Piska K, Satała G, Pęgiel J, Trybała W, Jastrzębska-Więsek M, Bojarski AJ, Lamaty F, Partyka A, Walczak M, Krawczyk M, Malikowska-Racia N, Popik P, Zajdel P. Grychowska K, et al. Eur J Med Chem. 2022 Jun 5;236:114329. doi: 10.1016/j.ejmech.2022.114329. Epub 2022 Mar 29. Eur J Med Chem. 2022. PMID: 35397400 Free article.
The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT₇ receptor antagonists.
Zajdel P, Kurczab R, Grychowska K, Satała G, Pawłowski M, Bojarski AJ. Zajdel P, et al. Among authors: grychowska k. Eur J Med Chem. 2012 Oct;56:348-60. doi: 10.1016/j.ejmech.2012.07.043. Epub 2012 Aug 4. Eur J Med Chem. 2012. PMID: 22926225
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
Pyrroloquinoline scaffold-based 5-HT6R ligands: Synthesis, quantum chemical and molecular dynamic studies, and influence of nitrogen atom position in the scaffold on affinity.
Grychowska K, Kurczab R, Śliwa P, Satała G, Dubiel K, Matłoka M, Moszczyński-Pętkowski R, Pieczykolan J, Bojarski AJ, Zajdel P. Grychowska K, et al. Bioorg Med Chem. 2018 Jul 23;26(12):3588-3595. doi: 10.1016/j.bmc.2018.05.033. Epub 2018 May 23. Bioorg Med Chem. 2018. PMID: 29853337
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. Among authors: grychowska k. 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.
Impact of the Substitution Pattern at the Basic Center and Geometry of the Amine Fragment on 5-HT6 and D3R Affinity in the 1H-Pyrrolo[3,2-c]quinoline Series.
Grychowska K, Pietruś W, Kulawik L, Bento O, Satała G, Bantreil X, Lamaty F, Bojarski AJ, Gołębiowska J, Nikiforuk A, Marin P, Chaumont-Dubel S, Kurczab R, Zajdel P. Grychowska K, et al. Molecules. 2023 Jan 21;28(3):1096. doi: 10.3390/molecules28031096. Molecules. 2023. PMID: 36770761 Free PMC article.
18 results