Novel pyrrolyl 2-aminopyridines as potent and selective human β-secretase (BACE1) inhibitors

Michael S. Malamas,Keith Barnes,Yu Hui,Matthew Johnson,Frank Lovering,Jeff Condon,William Fobare,William Solvibile,Jim Turner,Yun Hu,Eric S. Manas,Kristi Fan,Andrea Olland,Rajiv Chopra,Jonathan Bard,Menelas N. Pangalos,Peter Reinhart,Albert J. Robichaud

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

The 2-aminopyridine moiety is a bioisosteric replacement of the acylguanidine moiety with a lower Topological Polar Surface Area (TPSA) value and superior brain penetration.

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关键词

Alzheimer’s disease (AD),BACE1 inhibitors,Beta-amyloid peptide (Aβ),2-Aminopyridines

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