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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. 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.
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. 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
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: oehlrich d. 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
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: oehlrich d. 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
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: oehlrich d. 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
A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo.
Peschiulli A, Oehlrich D, Van Gool M, Austin N, Van Brandt S, Surkyn M, De Cleyn M, Vos A, Tresadern G, Rombouts FJR, Macdonald GJ, Moechars D, Trabanco AA, Gijsen HJM. Peschiulli A, et al. Among authors: oehlrich d. ACS Med Chem Lett. 2021 Dec 1;13(1):76-83. doi: 10.1021/acsmedchemlett.1c00445. eCollection 2022 Jan 13. ACS Med Chem Lett. 2021. PMID: 35059126 Free PMC article.
Scaffold hopping from pyridones to imidazo[1,2-a]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor.
Tresadern G, Cid JM, Macdonald GJ, Vega JA, de Lucas AI, García A, Matesanz E, Linares ML, Oehlrich D, Lavreysen H, Biesmans I, Trabanco AA. Tresadern G, et al. Among authors: oehlrich d. Bioorg Med Chem Lett. 2010 Jan 1;20(1):175-9. doi: 10.1016/j.bmcl.2009.11.008. Epub 2009 Nov 10. Bioorg Med Chem Lett. 2010. PMID: 19932615
39 results