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Expansion of the structure-activity relationships of BACE1 inhibitors by harnessing diverse building blocks prepared using a unified synthetic approach.

ABSTRACT: The structural diversity of ?-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors was expanded by harnessing diverse building blocks that had been prepared via a unified lead-oriented synthetic approach. It was shown that the lipophilic cyclohexylmethyl group within a known series of BACE1 inhibitors could be productively replaced with a range of alternative ring systems.

SUBMITTER: Mayol-Llinas J

PROVIDER: S-EPMC6482882 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature

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Expansion of the structure-activity relationships of BACE1 inhibitors by harnessing diverse building blocks prepared using a unified synthetic approach.

Mayol-Llinàs Joan J Chow Shiao S Nelson Adam A

MedChemComm 20190322 4

The structural diversity of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors was expanded by harnessing diverse building blocks that had been prepared <i>via</i> a unified lead-oriented synthetic approach. It was shown that the lipophilic cyclohexylmethyl group within a known series of BACE1 inhibitors could be productively replaced with a range of alternative ring systems. ...[more]

PMID: 31057741

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