This Letter details our efforts to develop novel tricyclic M 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 M receptor.
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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8648000 | PMC |
| http://dx.doi.org/10.1016/j.bmcl.2021.128416 | DOI Listing |
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