Bioorganic and Medicinal Chemistry Letters (2020)
Update date:2022-08-04
Topics:
Temple, Kayla J.
Engers, Julie L.
Long, Madeline F.
Watson, Katherine J.
Chang, Sichen
Luscombe, Vincent B.
Jenkins, Matthew T.
Rodriguez, Alice L.
Niswender, Colleen M.
Bridges, Thomas M.
Conn, P. Jeffrey
Engers, Darren W.
Lindsley, Craig W.
This Letter details our efforts to discover structurally unique M4 PAMs containing 5,6-heteroaryl ring systems. In an attempt to improve the DMPK profiles of the 2,3-dimethyl-2H-indazole-5-carboxamide and 1-methyl-1H-benzo[d][1,2,3]triazole-6-carboxamide cores, we investigated a plethora of core replacements. This exercise identified a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide core that provided improved M4 PAM activity and CNS penetration.
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