Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 19, Pages 5617-5622Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.08.042
Keywords
M5; mAChR; PAM; Allosteric
Categories
Funding
- NIMH [1RO1 MH082867]
- MLPCN [1U54 MH084659]
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This Letter describes a chemical lead optimization campaign directed at VU0238429, the first M-5-preferring positive allosteric modulator (PAM), discovered through analog work around VU0119498, a pan G(q) mAChR M-1, M-3, M-5 PAM. An iterative parallel synthesis approach was employed to incorporate basic heterocycles to improve physiochemical properties. (C) 2010 Elsevier Ltd. All rights reserved.
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