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Bioorg Med Chem Lett. 2013 May 15;23(10):3075-80. doi: 10.1016/j.bmcl.2013.03.009. Epub 2013 Mar 21.

Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors.

Author information

1
Department of Chemical Sciences, Elan Pharmaceuticals, 180 Oyster Point Boulevard, South San Francisco, CA 94080, USA. ying_zi_xu@yahoo.com

Abstract

Utilizing a structure based design approach, combined with extensive medicinal chemistry execution, highly selective, potent and novel BACE1 inhibitor 8 (BACE1 Alpha assay IC50=8nM) was made from a weak μM potency hit in an extremely efficient way. The detailed SAR and general design approaches will be discussed.

PMID:
23570791
DOI:
10.1016/j.bmcl.2013.03.009
[Indexed for MEDLINE]

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