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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: vos a. 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
Fragment Binding to β-Secretase 1 without Catalytic Aspartate Interactions Identified via Orthogonal Screening Approaches.
Rombouts FJR, Alexander R, Cleiren E, De Groot A, Carpentier M, Dijkmans J, Fierens K, Masure S, Moechars D, Palomino-Schätzlein M, Pineda-Lucena A, Trabanco AA, Van Glabbeek D, Vos A, Tresadern G. Rombouts FJR, et al. Among authors: vos a. ACS Omega. 2017 Feb 28;2(2):685-697. doi: 10.1021/acsomega.6b00482. Epub 2017 Feb 24. ACS Omega. 2017. PMID: 28626832 Free PMC article.
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: vos a. 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.
Discovery of 3-({5-Chloro-1-[3-(methylsulfonyl)propyl]-1H-indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-imidazo[4,5-c]pyridin-2-one (JNJ-53718678), a Potent and Orally Bioavailable Fusion Inhibitor of Respiratory Syncytial Virus.
Vendeville S, Tahri A, Hu L, Demin S, Cooymans L, Vos A, Kwanten L, Van den Berg J, Battles MB, McLellan JS, Koul A, Raboisson P, Roymans D, Jonckers THM. Vendeville S, et al. Among authors: vos a. J Med Chem. 2020 Aug 13;63(15):8046-8058. doi: 10.1021/acs.jmedchem.0c00226. Epub 2020 Jun 15. J Med Chem. 2020. PMID: 32407115
JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.
Rombouts FJR, Kusakabe KI, Alexander R, Austin N, Borghys H, De Cleyn M, Dhuyvetter D, Gijsen HJM, Hrupka B, Jacobs T, Jerhaoui S, Lammens L, Leclercq L, Tsubone K, Ueno T, Morimoto K, Einaru S, Sumiyoshi H, Van den Bergh A, Vos A, Surkyn M, Teisman A, Moechars D. Rombouts FJR, et al. Among authors: vos a. J Med Chem. 2021 Oct 14;64(19):14175-14191. doi: 10.1021/acs.jmedchem.1c00935. Epub 2021 Sep 23. J Med Chem. 2021. PMID: 34553934
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: vos a. 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.
1,144 results