PDE10A is a rather recently identified phosphodiesterase with a quite remarkable localization since the protein is abundant only in brain tissue. Based on this unique localization, research has focused extensively on using PDE10A modulators as a novel therapeutic approach for dysfunction in the basal ganglia circuit including Parkinson's disease, Huntington's disease, schizophrenia, addiction and obsessive compulsive disorder. Medicinal chemistry efforts identified the N-methyl-N-[4-(quinolin-2-ylmethoxy)-phenyl]-isonicotinamide (1  ) as a nanomolar PDE10A inhibitor. Herein we will present the syntheses and SAR of analogous N-methylanilides and their corresponding N-methylbenzamides (2)  .

N-Methylanilide and N-methylbenzamide derivatives as novel selective phosphodiesterase 10A (PDE10A) inhibitors

245th National Meeting (2013)

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