Discovery of structurally distinct tricyclic M4 positive allosteric modulator (PAM) chemotypes – Part 2
Bioorganic & Medicinal Chemistry Letters(2021)
摘要
This Letter details our efforts to develop novel tricyclic M4 PAM scaffolds with improved pharmacological properties. This endeavor involved a “tie-back” strategy to replace the 3-amino-4,6-dimethylthieno[2,3-b]pyridine-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 M4 receptor.
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关键词
M4,Muscarinic acetylcholine receptor,Positive Allosteric modulator (PAM),Structure Activity Relationship (SAR)
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