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Page 1
1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads.
Rombouts FJ, Tresadern G, Delgado O, Martínez-Lamenca C, Van Gool M, García-Molina A, Alonso de Diego SA, Oehlrich D, Prokopcova H, Alonso JM, Austin N, Borghys H, Van Brandt S, Surkyn M, De Cleyn M, Vos A, Alexander R, Macdonald G, Moechars D, Gijsen H, Trabanco AA. Rombouts FJ, et al. Among authors: austin n. J Med Chem. 2015 Oct 22;58(20):8216-35. doi: 10.1021/acs.jmedchem.5b01101. Epub 2015 Oct 10. J Med Chem. 2015. PMID: 26378740
Design and synthesis of trans-3-(2-(4-((3-(3-(5-methyl-1,2,4-oxadiazolyl))- phenyl)carboxamido)cyclohexyl)ethyl)-7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine (SB-414796): a potent and selective dopamine D3 receptor antagonist.
Macdonald GJ, Branch CL, Hadley MS, Johnson CN, Nash DJ, Smith AB, Stemp G, Thewlis KM, Vong AK, Austin NE, Jeffrey P, Winborn KY, Boyfield I, Hagan JJ, Middlemiss DN, Reavill C, Riley GJ, Watson JM, Wood M, Parker SG, Ashby CR Jr. Macdonald GJ, et al. Among authors: austin ne. J Med Chem. 2003 Nov 6;46(23):4952-64. doi: 10.1021/jm030817d. J Med Chem. 2003. PMID: 14584946
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
Kesteleyn B, Amssoms K, Schepens W, Hache G, Verschueren W, Van De Vreken W, Rombauts K, Meurs G, Sterkens P, Stoops B, Baert L, Austin N, Wegner J, Masungi C, Dierynck I, Lundgren S, Jönsson D, Parkes K, Kalayanov G, Wallberg H, Rosenquist A, Samuelsson B, Van Emelen K, Thuring JW. Kesteleyn B, et al. Among authors: austin n. Bioorg Med Chem Lett. 2013 Jan 1;23(1):310-7. doi: 10.1016/j.bmcl.2012.10.095. Epub 2012 Nov 1. Bioorg Med Chem Lett. 2013. PMID: 23177258
Discovery of N-(Pyridin-4-yl)-1,5-naphthyridin-2-amines as Potential Tau Pathology PET Tracers for Alzheimer's Disease.
Rombouts FJ, Andrés JI, Ariza M, Alonso JM, Austin N, Bottelbergs A, Chen L, Chupakhin V, Cleiren E, Fierens K, Fontana A, Langlois X, Leenaerts JE, Mariën J, Martínez Lamenca C, Salter R, Schmidt ME, Te Riele P, Wintmolders C, Trabanco AA, Zhang W, Macdonald G, Moechars D. Rombouts FJ, et al. Among authors: austin n. J Med Chem. 2017 Feb 23;60(4):1272-1291. doi: 10.1021/acs.jmedchem.6b01173. Epub 2017 Feb 10. J Med Chem. 2017. PMID: 28106992
Optimization of 1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.
Gijsen HJM, Alonso de Diego SA, De Cleyn M, García-Molina A, Macdonald GJ, Martínez-Lamenca C, Oehlrich D, Prokopcova H, Rombouts FJR, Surkyn M, Trabanco AA, Van Brandt S, Van den Bossche D, Van Gool M, Austin N, Borghys H, Dhuyvetter D, Moechars D. Gijsen HJM, et al. Among authors: austin n. J Med Chem. 2018 Jun 28;61(12):5292-5303. doi: 10.1021/acs.jmedchem.8b00304. Epub 2018 Jun 11. J Med Chem. 2018. PMID: 29809004
Correction to Optimization of 1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.
Gijsen HJM, Alonso de Diego SA, De Cleyn M, García-Molina A, Macdonald GJ, Martinez-Lamenca C, Oehlrich D, Prokopcova H, Rombouts FJR, Surkyn M, Trabanco AA, Van Brandt S, Van den Bossche D, Van Gool M, Austin N, Borghys H, Dhuyvetter D, Urmaliya V, Teisman A, Moechars D. Gijsen HJM, et al. Among authors: austin n. J Med Chem. 2018 Dec 27;61(24):11415. doi: 10.1021/acs.jmedchem.8b01859. Epub 2018 Dec 7. J Med Chem. 2018. PMID: 30525600 No abstract available.
Design and synthesis of a novel series of cyanoindole derivatives as potent γ-secretase modulators.
Bischoff FP, Velter AI, Minne G, Pieters S, Berthelot D, De Cleyn M, Gijsen HJM, Macdonald G, Surkyn M, Van Brandt S, Van Roosbroeck Y, Zavattaro C, Mercken M, Austin N, Dhuyvetter D, Borghys H, Ahmad I, Samanta SK. Bischoff FP, et al. Among authors: austin n. Bioorg Med Chem Lett. 2019 Jul 15;29(14):1737-1745. doi: 10.1016/j.bmcl.2019.05.023. Epub 2019 May 15. Bioorg Med Chem Lett. 2019. PMID: 31122869
Evaluation of a Series of β-Secretase 1 Inhibitors Containing Novel Heteroaryl-Fused-Piperazine Amidine Warheads.
Oehlrich D, Peschiulli A, Tresadern G, Van Gool M, Vega JA, De Lucas AI, Alonso de Diego SA, Prokopcova H, Austin N, Van Brandt S, Surkyn M, De Cleyn M, Vos A, Rombouts FJR, Macdonald G, Moechars D, Gijsen HJM, Trabanco AA. Oehlrich D, et al. Among authors: austin n. ACS Med Chem Lett. 2019 Jul 2;10(8):1159-1165. doi: 10.1021/acsmedchemlett.9b00181. eCollection 2019 Aug 8. ACS Med Chem Lett. 2019. PMID: 31413800 Free PMC article.
233 results