Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 53, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2021.128416
Keywords
M-4; Muscarinic acetylcholine receptor; Positive Allosteric modulator (PAM); Structure Activity Relationship (SAR)
Categories
Funding
- NIH via the NIH Roadmap Initiative [1X01 MH077607]
- Molecular Libraries Probe Center Network [U54MH084659]
- William K. Warren Foundation
- Vanderbilt NCDDG [U01MH087965]
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The Letter details efforts to develop novel tricyclic M-4 PAM scaffolds with improved pharmacological properties. A tie-back strategy was employed to replace the core structure, leading to the discovery of two novel tricyclic cores with low nanomolar potency against the human M-4 receptor.
This Letter details our efforts to develop novel tricyclic M-4 PAM scaffolds with improved pharmacological properties. This endeavor involved a tie-back strategy to replace the 3-amino-4,6-dimethylthieno[2,3-b]pyri-dine-2-carboxamide core which lead to the discovery of two novel tricyclic cores: a 7,9-dimethylpyrido[3 ',2 ':4,5] thieno[3,2-d]pyrimidine core and 2,4-dimethylthieno[2,3-b:5,4-c ']dipyridine core. Both tricyclic cores displayed low nanomolar potency against the human M-4 receptor.
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