期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 2, 页码 632-635出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.11.052
关键词
BACE1; Aminohydantoin; Alzheimer's disease
8,8-Diphenyl-2,3,4,8-tetrahydroimidazo[1,5-a] pyrimidin-6-amine (1) was identified through HTS, as a weak (micromolar) inhibitor of BACE1. X-Ray crystallographic studies indicate the 2-aminoimidazole ring forms key H-bonding interactions with Asp32 and Asp228 in the catalytic site of BACE1. Lead optimization using structure-based focused libraries led to the identification of low nanomolar BACE1 inhibitors such as 20b with substituents which extend from the S(1) to the S(3) pocket. (C) 2009 Elsevier Ltd. All rights reserved.
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