New evolutions in the BACE1 inhibitor field from 2014 to 2018

Bioorg Med Chem Lett. 2019 Mar 15;29(6):761-777. doi: 10.1016/j.bmcl.2018.12.049.

Chien-Chi Hsiao ¹, Frederik Rombouts ², Harrie J M Gijsen ²

Affiliations

1 Janssen Research & Development, Janssen Pharmaceutica N. V, Turnhoutseweg 30, B-2340 Beerse, Belgium. Electronic address: mhsiao3@its.jnj.com.
2 Janssen Research & Development, Janssen Pharmaceutica N. V, Turnhoutseweg 30, B-2340 Beerse, Belgium.

PMID: 30709653 DOI: 10.1016/j.bmcl.2018.12.049

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.

Keywords

Alzheimer’s; Amidine; Amyloid; BACE; BACE1; Inhibitor; Neurodegenerative diseases.

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