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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. Among authors: moechars d. 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.
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: moechars 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
Rational design and synthesis of aminopiperazinones as β-secretase (BACE) inhibitors.
Tresadern G, Delgado F, Delgado O, Gijsen H, Macdonald GJ, Moechars D, Rombouts F, Alexander R, Spurlino J, Van Gool M, Vega JA, Trabanco AA. Tresadern G, et al. Among authors: moechars d. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7255-60. doi: 10.1016/j.bmcl.2011.10.050. Epub 2011 Oct 20. Bioorg Med Chem Lett. 2011. PMID: 22071305
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: moechars d. 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
BACE2 distribution in major brain cell types and identification of novel substrates.
Voytyuk I, Mueller SA, Herber J, Snellinx A, Moechars D, van Loo G, Lichtenthaler SF, De Strooper B. Voytyuk I, et al. Among authors: moechars d. Life Sci Alliance. 2018 Feb 15;1(1):e201800026. doi: 10.26508/lsa.201800026. eCollection 2018 Jan. Life Sci Alliance. 2018. PMID: 30456346 Free PMC article.
Preclinical evaluation of 18F-JNJ41510417 as a radioligand for PET imaging of phosphodiesterase-10A in the brain.
Celen S, Koole M, De Angelis M, Sannen I, Chitneni SK, Alcazar J, Dedeurwaerdere S, Moechars D, Schmidt M, Verbruggen A, Langlois X, Van Laere K, Andrés JI, Bormans G. Celen S, et al. Among authors: moechars d. J Nucl Med. 2010 Oct;51(10):1584-91. doi: 10.2967/jnumed.110.077040. Epub 2010 Sep 16. J Nucl Med. 2010. PMID: 20847170 Free article.
118 results