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Paradoxical Increase of Permeability and Lipophilicity with the Increasing Topological Polar Surface Area within a Series of PRMT5 Inhibitors.
Argikar U, Blatter M, Bednarczyk D, Chen Z, Cho YS, Doré M, Dumouchel JL, Ho S, Hoegenauer K, Kawanami T, Mathieu S, Meredith E, Möbitz H, Murphy SK, Parthasarathy S, Soldermann CP, Santos J, Silver S, Skolnik S, Stojanovic A. Argikar U, et al. Among authors: bednarczyk d. J Med Chem. 2022 Sep 22;65(18):12386-12402. doi: 10.1021/acs.jmedchem.2c01068. Epub 2022 Sep 7. J Med Chem. 2022. PMID: 36069672
Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition.
Fu J, Tjandra M, Becker C, Bednarczyk D, Capparelli M, Elling R, Hanna I, Fujimoto R, Furegati M, Karur S, Kasprzyk T, Knapp M, Leung K, Li X, Lu P, Mergo W, Miault C, Ng S, Parker D, Peng Y, Roggo S, Rivkin A, Simmons RL, Wang M, Wiedmann B, Weiss AH, Xiao L, Xie L, Xu W, Yifru A, Yang S, Zhou B, Sweeney ZK. Fu J, et al. Among authors: bednarczyk d. J Med Chem. 2014 Oct 23;57(20):8503-16. doi: 10.1021/jm500862r. Epub 2014 Oct 13. J Med Chem. 2014. PMID: 25310383
Unbound Brain-to-Plasma Partition Coefficient, Kp,uu,brain-a Game Changing Parameter for CNS Drug Discovery and Development.
Loryan I, Reichel A, Feng B, Bundgaard C, Shaffer C, Kalvass C, Bednarczyk D, Morrison D, Lesuisse D, Hoppe E, Terstappen GC, Fischer H, Di L, Colclough N, Summerfield S, Buckley ST, Maurer TS, Fridén M. Loryan I, et al. Among authors: bednarczyk d. Pharm Res. 2022 Jul;39(7):1321-1341. doi: 10.1007/s11095-022-03246-6. Epub 2022 Apr 11. Pharm Res. 2022. PMID: 35411506 Free PMC article.
50 results