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Publikationer i urvalet

11 träffar

Bibliografisk träff 2021-11-24

Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors.

Taoka BM, Wu WL, Hao J, Dolmaski M, Wang H, Levorse D, Orth P, Hyde LA, Smith B, Michener MS, Kennedy ME, Parker EM, Cumming JN.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2021.128463

Bibliografisk träff 2021-09-23

Discovery of Extremely Selective Fused Pyridine-Derived β-Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions.

Ueno T, Matsuoka E, Asada N, Yamamoto S, Kanegawa N, Ito M, Ito H, Moechars D, Rombouts FJR, Gijsen HJM, Kusakabe KI.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.1c00359

Bibliografisk träff 2021-04-07

Synthesis and evaluation of multi-target-directed ligands with BACE-1 inhibitory and Nrf2 agonist activities as potential agents against Alzheimer's disease.

Qu L, Ji L, Wang C, Luo H, Li S, Peng W, Yin F, Lu D, Liu X, Kong L, Wang X.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2021.113441

Bibliografisk träff 2021-03-15

Structure-Based Approaches to Improving Selectivity through Utilizing Explicit Water Molecules: Discovery of Selective β-Secretase (BACE1) Inhibitors over BACE2.

Fujimoto K, Yoshida S, Tadano G, Asada N, Fuchino K, Suzuki S, Matsuoka E, Yamamoto T, Yamamoto S, Ando S, Kanegawa N, Tonomura Y, Ito H, Moechars D, Rombouts FJR, Gijsen HJM, Kusakabe KI.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.0c01858

Bibliografisk träff 2020-12-21

Glycogen Synthase Kinase 3β: A New Gold Rush in Anti-Alzheimer's Disease Multitarget Drug Discovery?

De Simone A, Tumiatti V, Andrisano V, Milelli A.

J Med Chem · research support, non-u.s. gov't; review-article; journal article · DOI 10.1021/acs.jmedchem.0c00931

Bibliografisk träff 2019-10-08

Discovery of an Extremely Potent Thiazine-Based β-Secretase Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose.

Tadano G, Komano K, Yoshida S, Suzuki S, Nakahara K, Fuchino K, Fujimoto K, Matsuoka E, Yamamoto T, Asada N, Ito H, Sakaguchi G, Kanegawa N, Kido Y, Ando S, Fukushima T, Teisman A, Urmaliya V, Dhuyvetter D, Borghys H, Van Den Bergh A, Austin N, Gijsen HJM, Yamano Y, Iso Y, Kusakabe KI.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.9b01140

Bibliografisk träff 2019-02-04

Synthesis and evaluation of tetrahydroisoquinoline-benzimidazole hybrids as multifunctional agents for the treatment of Alzheimer's disease.

Fang Y, Zhou H, Gu Q, Xu J.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2019.02.008

Bibliografisk träff 2019-01-04

New evolutions in the BACE1 inhibitor field from 2014 to 2018.

Hsiao CC, Rombouts F, Gijsen HJM.

Bioorg Med Chem Lett · review; journal article · DOI 10.1016/j.bmcl.2018.12.049

Bibliografisk träff 2018-04-25

Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.

Young RJ, Leeson PD.

J Med Chem · review; journal article · DOI 10.1021/acs.jmedchem.8b00180

Bibliografisk träff 2018-04-17

Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.

O'Neill BT, Beck EM, Butler CR, Nolan CE, Gonzales C, Zhang L, Doran SD, Lapham K, Buzon LM, Dutra JK, Barreiro G, Hou X, Martinez-Alsina LA, Rogers BN, Villalobos A, Murray JC, Ogilvie K, LaChapelle EA, Chang C, Lanyon LF, Steppan CM, Robshaw A, Hales K, Boucher GG, Pandher K, Houle C, Ambroise CW, Karanian D, Riddell D, Bales KR, Brodney MA.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.8b00246

Bibliografisk träff 2017-06-24

Discovery of imidazopyridines containing isoindoline-1,3-dione framework as a new class of BACE1 inhibitors: Design, synthesis and SAR analysis.

Azimi S, Zonouzi A, Firuzi O, Iraji A, Saeedi M, Mahdavi M, Mahdavi M, Edraki N.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2017.06.040