Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.

Abstract:

:Based on lead compound 1 identified from the patent literature, we developed novel patentable BACE-1 inhibitors by introducing a cyclic amine scaffold. Extensive SAR studies on both pyrrolidines and piperidines ultimately led to inhibitor 2f, one of the most potent inhibitors synthesized to date.

journal_name

Bioorg Med Chem Lett

authors

Iserloh U,Wu Y,Cumming JN,Pan J,Wang LY,Stamford AW,Kennedy ME,Kuvelkar R,Chen X,Parker EM,Strickland C,Voigt J

doi

10.1016/j.bmcl.2007.10.116

subject

Has Abstract

pub_date

2008-01-01 00:00:00

pages

414-7

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)01316-9

journal_volume

18

pub_type

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