Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M4 positive allosteric modulator (PAM) chemotype.

Kayla J Temple,Julie L Engers,Madeline F Long,Katherine J Watson,Sichen Chang,Vincent B Luscombe,Matthew T Jenkins,Alice L Rodriguez,Colleen M Niswender,Thomas M Bridges,P Jeffrey Conn,Darren W Engers,Craig W Lindsley

Bioorganic & medicinal chemistry letters（2019）

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摘要

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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