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Hybrid molecules combining GABA-A and serotonin 5-HT6 receptors activity designed to tackle neuroinflammation associated with depression.
Marcinkowska M, Mordyl B, Fajkis-Zajaczkowska N, Siwek A, Karcz T, Gawalska A, Bucki A, Żmudzki P, Partyka A, Jastrzębska-Więsek M, Pomierny B, Walczak M, Smolik M, Pytka K, Mika K, Kotańska M, Kolaczkowski M. Marcinkowska M, et al. Eur J Med Chem. 2023 Feb 5;247:115071. doi: 10.1016/j.ejmech.2022.115071. Epub 2022 Dec 29. Eur J Med Chem. 2023. PMID: 36603509
Dual Piperidine-Based Histamine H3 and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain.
Szczepańska K, Karcz T, Dichiara M, Mogilski S, Kalinowska-Tłuścik J, Pilarski B, Leniak A, Pietruś W, Podlewska S, Popiołek-Barczyk K, Humphrys LJ, Ruiz-Cantero MC, Reiner-Link D, Leitzbach L, Łażewska D, Pockes S, Górka M, Zmysłowski A, Calmels T, Cobos EJ, Marrazzo A, Stark H, Bojarski AJ, Amata E, Kieć-Kononowicz K. Szczepańska K, et al. J Med Chem. 2023 Jul 27;66(14):9658-9683. doi: 10.1021/acs.jmedchem.3c00430. Epub 2023 Jul 7. J Med Chem. 2023. PMID: 37418295 Free PMC article.
First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT6 Agents with a Beneficial Neuroprotective Profile against Alzheimer's Disease.
Pyka P, Haberek W, Więcek M, Szymanska E, Ali W, Cios A, Jastrzębska-Więsek M, Satała G, Podlewska S, Di Giacomo S, Di Sotto A, Garbo S, Karcz T, Lambona C, Marocco F, Latacz G, Sudoł-Tałaj S, Mordyl B, Głuch-Lutwin M, Siwek A, Czarnota-Łydka K, Gogola D, Olejarz-Maciej A, Wilczyńska-Zawal N, Honkisz-Orzechowska E, Starek M, Dąbrowska M, Kucwaj-Brysz K, Fioravanti R, Nasim MJ, Hittinger M, Partyka A, Wesołowska A, Battistelli C, Zwergel C, Handzlik J. Pyka P, et al. J Med Chem. 2024 Jan 25;67(2):1580-1610. doi: 10.1021/acs.jmedchem.3c02148. Epub 2024 Jan 8. J Med Chem. 2024. PMID: 38190615 Free PMC article.
Discovery of novel arylpiperazine-based DA/5-HT modulators as potential antipsychotic agents - Design, synthesis, structural studies and pharmacological profiling.
Stępnicki P, Targowska-Duda KM, Martínez AL, Zięba A, Wronikowska-Denysiuk O, Wróbel MZ, Bartyzel A, Trzpil A, Wróbel TM, Chodkowski A, Mirecka K, Karcz T, Szczepańska K, Loza MI, Budzyńska B, Turło J, Handzlik J, Fornal E, Poleszak E, Castro M, Kaczor AA. Stępnicki P, et al. Eur J Med Chem. 2023 Apr 5;252:115285. doi: 10.1016/j.ejmech.2023.115285. Epub 2023 Mar 17. Eur J Med Chem. 2023. PMID: 37027998
Dual 5-HT6/SERT ligands for mitigating neuropsychiatric symptoms of dementia exerting neuroprotection against amyloid-β toxicity, memory preservation, and antidepressant-like properties.
Siwek A, Marcinkowska M, Głuch-Lutwin M, Mordyl B, Wolak M, Jastrzębska-Więsek M, Wilczyńska-Zawal N, Wyska E, Szafrańska K, Karcz T, Ostrowska O, Bucki A, Kołaczkowski M. Siwek A, et al. Eur J Med Chem. 2024 Sep 5;275:116601. doi: 10.1016/j.ejmech.2024.116601. Epub 2024 Jun 14. Eur J Med Chem. 2024. PMID: 38901106
Structure-Activity Relationship of Heterocyclic P2Y14 Receptor Antagonists: Removal of the Zwitterionic Character with Piperidine Bioisosteres.
Jung YH, Salmaso V, Wen Z, Bennett JM, Phung NB, Lieberman DI, Gopinatth V, Randle JCR, Chen Z, Salvemini D, Karcz TP, Cook DN, Jacobson KA. Jung YH, et al. Among authors: karcz tp. J Med Chem. 2021 Apr 22;64(8):5099-5122. doi: 10.1021/acs.jmedchem.1c00164. Epub 2021 Mar 31. J Med Chem. 2021. PMID: 33787273 Free PMC article.
55 results