New evolutions in the BACE1 inhibitor field from 2014 to 2018 |
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Authors: | Chien-Chi Hsiao Frederik Rombouts Harrie J.M. Gijsen |
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Affiliation: | Janssen Research & Development, Janssen Pharmaceutica N. V, Turnhoutseweg 30, B-2340 Beerse, Belgium |
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Abstract: | β-Site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors offer the potential of disease-modifying treatment for Alzheimer’s disease (AD). Since 2014, major breakthroughs have appeared in the field of BACE1 inhibitors. This review provides an overview of amidine-based BACE1 inhibitors between 2014 and 2018. Herein are summarized i) the structure-activity relationship, ii) the physiological results and iii) the potential risks from a lack of selectivity. This review also summarizes clinical scope, results and outlook of the compounds that have been or are currently under development in clinical trials. |
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Keywords: | Alzheimer’s BACE BACE1 Inhibitor Amyloid Neurodegenerative diseases Amidine |
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