Acylguanidine inhibitors of [beta]-secretase: Optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets (original) (raw)

Acylguanidine inhibitors of [beta]-secretase: Optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets

Bioorganic & medicinal …, 2008

Abstract

Proteolytic cleavage of amyloid precursor protein by β-secretase (BACE-1) and γ-secretase leads to formation of β-amyloid (Aβ) a key component of amyloid plaques, which are considered the hallmark of Alzheimer's disease. Small molecule inhibitors of BACE-1 may reduce levels ...

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