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Brain-penetrant cyanoindane and cyanotetralin inhibitors of G2019S-LRRK2 kinase activity.
Garofalo AW, Schwarz J, Zobel K, Beato C, Bernardi S, Budassi F, Caberlotto L, Gao P, Griffante C, Liu X, Migliore M, Qiao F, Sabbatini FM, Sava A, Zhang M, Carlisle HJ. Garofalo AW, et al. Among authors: griffante c. Bioorg Med Chem Lett. 2023 Oct 15;95:129487. doi: 10.1016/j.bmcl.2023.129487. Epub 2023 Sep 19. Bioorg Med Chem Lett. 2023. PMID: 37734423
Selective Inhibitors of G2019S-LRRK2 Kinase Activity.
Garofalo AW, Bright J, De Lombaert S, Toda AMA, Zobel K, Andreotti D, Beato C, Bernardi S, Budassi F, Caberlotto L, Gao P, Griffante C, Liu X, Mengatto L, Migliore M, Sabbatini FM, Sava A, Serra E, Vincetti P, Zhang M, Carlisle HJ. Garofalo AW, et al. Among authors: griffante c. J Med Chem. 2020 Dec 10;63(23):14821-14839. doi: 10.1021/acs.jmedchem.0c01243. Epub 2020 Nov 16. J Med Chem. 2020. PMID: 33197196
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
Di Fabio R, Griffante C, Alvaro G, Pentassuglia G, Pizzi DA, Donati D, Rossi T, Guercio G, Mattioli M, Cimarosti Z, Marchioro C, Provera S, Zonzini L, Montanari D, Melotto S, Gerrard PA, Trist DG, Ratti E, Corsi M. Di Fabio R, et al. Among authors: griffante c. J Med Chem. 2009 May 28;52(10):3238-47. doi: 10.1021/jm900023b. J Med Chem. 2009. PMID: 19388677
Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.
Sabbatini FM, Di Fabio R, Griffante C, Pentassuglia G, Zonzini L, Melotto S, Alvaro G, Capelli AM, Pippo L, Perdona' E, St Denis Y, Costa S, Corsi M. Sabbatini FM, et al. Among authors: griffante c. Bioorg Med Chem Lett. 2010 Jan 15;20(2):623-7. doi: 10.1016/j.bmcl.2009.11.078. Epub 2009 Nov 20. Bioorg Med Chem Lett. 2010. PMID: 19963378
Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clinical candidate.
Di Fabio R, Alvaro G, Griffante C, Pizzi DA, Donati D, Mattioli M, Cimarosti Z, Guercio G, Marchioro C, Provera S, Zonzini L, Montanari D, Melotto S, Gerrard PA, Trist DG, Ratti E, Corsi M. Di Fabio R, et al. Among authors: griffante c. J Med Chem. 2011 Feb 24;54(4):1071-9. doi: 10.1021/jm1013264. Epub 2011 Jan 13. J Med Chem. 2011. PMID: 21229983
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