Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.

Wood MR, Noetzel MJ, Engers JL, Bollinger KA, Melancon BJ, Tarr JC, Han C, West M, Gregro AR, Lamsal A, Chang S, Ajmera S, Smith E, Chase P, Hodder PS, Bubser M, Jones CK, Hopkins CR, Emmitte KA, Niswender CM, Wood MW, Duggan ME, Conn PJ, Bridges TM, Lindsley CW
Bioorg Med Chem Lett. 2016 26 (13): 3029-3033

PMID: 27185330 · PMCID: PMC4955361 · DOI:10.1016/j.bmcl.2016.05.010

MeSH Terms (12)

Allosteric Regulation Animals Brain Humans Microsomes, Liver Piperidines Pyrimidines Quinazolines Rats Receptor, Muscarinic M4 Structure-Activity Relationship Thiophenes

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