期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 9, 页码 2697-2701出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.12.015
关键词
Muscarinic; Acetylcholine; Positive allosteric modulator (PAM); ML169; BQCA; Alzheimer's disease; MLPCN
资金
- MLPCN [1U54 MH084659]
- NIMH [1RO1 MH082867]
- NIH
- Alzheimer's Association [IIRG-07-57131]
This Letter describes a chemical lead optimization campaign directed at VU0108370, a weak M-1 PAM hit with a novel chemical scaffold from a functional HTS screen within the MLPCN. An iterative parallel synthesis approach rapidly established SAR for this series and afforded VU0405652 (ML169), a potent, selective and brain penetrant M-1 PAM with an in vitro profile comparable to the prototypical M-1 PAM, BQCA, but with an improved brain to plasma ratio. (C) 2010 Elsevier Ltd. All rights reserved.
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