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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. Among authors: blicharz k. 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.
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: blicharz 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
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. Among authors: blicharz k. 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