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Daedalols A-C, fungal-derived BACE1 inhibitors.

ABSTRACT: Bioassay-guided fractionation of an extract prepared from the fruiting bodies of a Daedalea sp. has led to the isolation of daedalols A-C (1-3). The structures of these new triterpenes were elucidated based on extensive NMR spectroscopic and mass spectrometric measurements. Assignment of the relative configuration of 3 required the preparation of a suitable derivative via a Payne rearrangement. The aspartic protease BACE1, an Alzheimer's drug target, was inhibited by 3 with an IC(50) value of 14.2 ?M.

SUBMITTER: Sorribas A

PROVIDER: S-EPMC3209533 | biostudies-literature | 2011 Nov

REPOSITORIES: biostudies-literature

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Daedalols A-C, fungal-derived BACE1 inhibitors.

Sorribas Analia A Jiménez Jorge I JI Yoshida Wesley Y WY Williams Philip G PG

Bioorganic & medicinal chemistry 20110922 22

Bioassay-guided fractionation of an extract prepared from the fruiting bodies of a Daedalea sp. has led to the isolation of daedalols A-C (1-3). The structures of these new triterpenes were elucidated based on extensive NMR spectroscopic and mass spectrometric measurements. Assignment of the relative configuration of 3 required the preparation of a suitable derivative via a Payne rearrangement. The aspartic protease BACE1, an Alzheimer's drug target, was inhibited by 3 with an IC(50) value of 14 ...[more]

PMID: 21992804

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