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New aminoimidazoles as β-secretase (BACE-1) inhibitors showing amyloid-β (Aβ) lowering in brain.
Gravenfors Y, Viklund J, Blid J, Ginman T, Karlström S, Kihlström J, Kolmodin K, Lindström J, von Berg S, von Kieseritzky F, Bogar K, Slivo C, Swahn BM, Olsson LL, Johansson P, Eketjäll S, Fälting J, Jeppsson F, Strömberg K, Janson J, Rahm F. Gravenfors Y, et al. Among authors: swahn bm. J Med Chem. 2012 Nov 8;55(21):9297-311. doi: 10.1021/jm300991n. Epub 2012 Oct 3. J Med Chem. 2012. PMID: 23017051
Aminoimidazoles as BACE-1 inhibitors: the challenge to achieve in vivo brain efficacy.
Swahn BM, Holenz J, Kihlström J, Kolmodin K, Lindström J, Plobeck N, Rotticci D, Sehgelmeble F, Sundström M, Berg Sv, Fälting J, Georgievska B, Gustavsson S, Neelissen J, Ek M, Olsson LL, Berg S. Swahn BM, et al. Bioorg Med Chem Lett. 2012 Mar 1;22(5):1854-9. doi: 10.1016/j.bmcl.2012.01.079. Epub 2012 Jan 28. Bioorg Med Chem Lett. 2012. PMID: 22325942
Design and synthesis of β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction of β-amyloid peptides.
Swahn BM, Kolmodin K, Karlström S, von Berg S, Söderman P, Holenz J, Berg S, Lindström J, Sundström M, Turek D, Kihlström J, Slivo C, Andersson L, Pyring D, Rotticci D, Ohberg L, Kers A, Bogar K, von Kieseritzky F, Bergh M, Olsson LL, Janson J, Eketjäll S, Georgievska B, Jeppsson F, Fälting J. Swahn BM, et al. J Med Chem. 2012 Nov 8;55(21):9346-61. doi: 10.1021/jm3009025. Epub 2012 Sep 17. J Med Chem. 2012. PMID: 22924815
Discovery of AZD3839, a potent and selective BACE1 inhibitor clinical candidate for the treatment of Alzheimer disease.
Jeppsson F, Eketjäll S, Janson J, Karlström S, Gustavsson S, Olsson LL, Radesäter AC, Ploeger B, Cebers G, Kolmodin K, Swahn BM, von Berg S, Bueters T, Fälting J. Jeppsson F, et al. Among authors: swahn bm. J Biol Chem. 2012 Nov 30;287(49):41245-57. doi: 10.1074/jbc.M112.409110. Epub 2012 Oct 9. J Biol Chem. 2012. PMID: 23048024 Free PMC article.
AZ-4217: a high potency BACE inhibitor displaying acute central efficacy in different in vivo models and reduced amyloid deposition in Tg2576 mice.
Eketjäll S, Janson J, Jeppsson F, Svanhagen A, Kolmodin K, Gustavsson S, Radesäter AC, Eliason K, Briem S, Appelkvist P, Niva C, Berg AL, Karlström S, Swahn BM, Fälting J. Eketjäll S, et al. Among authors: swahn bm. J Neurosci. 2013 Jun 12;33(24):10075-84. doi: 10.1523/JNEUROSCI.1165-13.2013. J Neurosci. 2013. PMID: 23761903 Free PMC article.
Synthesis and evaluation of 2-pyridylbenzothiazole, 2-pyridylbenzoxazole and 2-pyridylbenzofuran derivatives as 11C-PET imaging agents for beta-amyloid plaques.
Swahn BM, Wensbo D, Sandell J, Sohn D, Slivo C, Pyring D, Malmström J, Arzel E, Vallin M, Bergh M, Jeppsson F, Johnson AE, Juréus A, Neelissen J, Svensson S. Swahn BM, et al. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1976-80. doi: 10.1016/j.bmcl.2010.01.105. Epub 2010 Jan 25. Bioorg Med Chem Lett. 2010. PMID: 20153963
17 results