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. 2013 Dec 15;21(24):7612-23.
doi: 10.1016/j.bmc.2013.10.035. Epub 2013 Oct 31.

Design and synthesis of novel benzimidazole derivatives as phosphodiesterase 10A inhibitors with reduced CYP1A2 inhibition

Wataru Hamaguchi  1 , Naoyuki Masuda, Mai Isomura, Satoshi Miyamoto, Shigetoshi Kikuchi, Yasushi Amano, Kazuya Honbou, Takuma Mihara, Toshihiro Watanabe
Affiliations

Design and synthesis of novel benzimidazole derivatives as phosphodiesterase 10A inhibitors with reduced CYP1A2 inhibition

Wataru Hamaguchi et al. Bioorg Med Chem. .

Abstract

A novel class of phosphodiesterase 10A (PDE10A) inhibitors with reduced CYP1A2 inhibition were designed and synthesized starting from 2-{[(1-phenyl-1H-benzimidazol-6-yl)oxy]methyl}quinoline (1). Introduction of an isopropyl group at the 2-position and a methoxy group at the 5-position of the benzimidazole ring of lead compound 1 resulted in the identification of 2-{[(2-isopropyl-5-methoxy-1-phenyl-1H-benzimidazol-6-yl)oxy]methyl}quinoline (25b), which exhibited potent PDE10A inhibitory activity with reduced CYP1A2 inhibitory activity compared to compound 1.

Keywords: Benzimidazole; CYP1A2; PDE10A inhibitor; Schizophrenia.

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