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2-Amino-3,4-dihydroquinazolines as inhibitors of BACE-1 (beta-site APP cleaving enzyme): Use of structure based design to convert a micromolar hit into a nanomolar lead.
Baxter EW, Conway KA, Kennis L, Bischoff F, Mercken MH, Winter HL, Reynolds CH, Tounge BA, Luo C, Scott MK, Huang Y, Braeken M, Pieters SM, Berthelot DJ, Masure S, Bruinzeel WD, Jordan AD, Parker MH, Boyd RE, Qu J, Alexander RS, Brenneman DE, Reitz AB. Baxter EW, et al. J Med Chem. 2007 Sep 6;50(18):4261-4. doi: 10.1021/jm0705408. Epub 2007 Aug 8. J Med Chem. 2007. PMID: 17685503
Design and synthesis of bicyclic heterocycles as potent γ-secretase modulators.
Oehlrich D, Rombouts FJ, Berthelot D, Bischoff FP, De Cleyn MA, Jaroskova L, Macdonald G, Mercken M, Surkyn M, Trabanco AA, Tresadern G, Van Brandt S, Velter AI, Wu T, Gijsen HJ. Oehlrich D, et al. Among authors: bischoff fp. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4794-800. doi: 10.1016/j.bmcl.2013.06.100. Epub 2013 Jul 11. Bioorg Med Chem Lett. 2013. PMID: 23890837
Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.
Letavic MA, Lord B, Bischoff F, Hawryluk NA, Pieters S, Rech JC, Sales Z, Velter AI, Ao H, Bonaventure P, Contreras V, Jiang X, Morton KL, Scott B, Wang Q, Wickenden AD, Carruthers NI, Bhattacharya A. Letavic MA, et al. ACS Med Chem Lett. 2013 Mar 12;4(4):419-22. doi: 10.1021/ml400040v. eCollection 2013 Apr 11. ACS Med Chem Lett. 2013. PMID: 24900687 Free PMC article.
Anilinotriazoles as potent gamma secretase modulators.
Velter AI, Bischoff FP, Berthelot D, De Cleyn M, Oehlrich D, Jaroskova L, Macdonald G, Minne G, Pieters S, Rombouts F, Van Brandt S, Van Roosbroeck Y, Surkyn M, Trabanco AA, Tresadern G, Wu T, Borghys H, Mercken M, Masungi C, Gijsen H. Velter AI, et al. Among authors: bischoff fp. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5805-5813. doi: 10.1016/j.bmcl.2014.10.024. Epub 2014 Oct 18. Bioorg Med Chem Lett. 2014. PMID: 25454273
20 results