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Discovery of a series of selective and cell permeable beta-secretase (BACE1) inhibitors by fragment linking with the assistance of STD-NMR.

Abstract：

:Two β-secreatase (BACE1) inhibitors from natural products (cinnamic acid and flavone) were linked to furnish potent, cell permeable BACE1 inhibitors with noncompetitive mode of inhibition, with the assistance of saturated transfer difference (STD)-NMR technique. Some of these conjugates also exhibited selective BACE1 inhibition over other aspartyl proteases such as BACE-2 and renin, as well as poor cytotoxicity. Taken together, conjugates 4 represent a new series of BACE inhibitors warrants further investigation for their potential in Alzheimier's disease therapy.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Fang WS,Sun DY,Yang S,Cheng C,Moschke K,Li T,Sun S,Lichtenthaler SF,Huang J,Wang Y

doi

10.1016/j.bioorg.2019.103253

subject

Has Abstract

pub_date

2019-11-01 00:00:00

pages

103253

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(19)30079-3

journal_volume

92

pub_type

杂志文章

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