Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 29, Issue 21, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.126678
Keywords
M-4; Muscarinic acetylcholine receptor; Positive allosteric modulator (PAM); Structure activity relationship (SAR)
Categories
Funding
- NIH via NIH Roadmap Initiative [1x01 MH077607]
- Molecular Libraries Probe Center Network [U54MH084659, U01MH087965]
- William K. Warren Foundation
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This Letter details our efforts to replace the 2,4-dimethylquinoline carboxamide core of our previous M-4 PAM series, which suffered from high predicted hepatic clearance and protein binding. A scaffold hopping exercise identified a novel 3,4-dimethylcinnoline carboxamide core that provided good M-4 PAM activity and improved clearance and protein binding profiles.
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