期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 16, 页码 4354-4359出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.05.046
关键词
Alzheimer's disease; BACE1 inhibitor; cultured cells
Recently, we reported potent and small-sized P-secretase (BACE1) inhibitors KMI-570 and KMI-684 in which we replaced carboxylic acid groups at the P-1(') position of KMI-420 and KMI-429, respectively, with tetrazole derivatives as carboxylic acid bioisosteres. These modifications improved significantly BACE1 inhibitory activity and chemical stability. In this study, the acidic tetrazole ring of the P-4 position of KMI-420 and KMI-570, respectively, was replaced with various hydrogen bond acceptor groups. We found BACE1 inhibitor KMI-574 that exhibited potent inhibitory activity in cultured cells as well as in vitro enzymatic assay. (c) 2006 Elsevier Ltd. All rights reserved.
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