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PDBsum entry 3wi2
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Hydrolase/hydrolase inhibitor
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PDB id
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3wi2
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References listed in PDB file
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Key reference
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Title
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Design and synthesis of novel benzimidazole derivatives as phosphodiesterase 10a inhibitors with reduced cyp1a2 inhibition.
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Authors
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W.Hamaguchi,
N.Masuda,
M.Isomura,
S.Miyamoto,
S.Kikuchi,
Y.Amano,
K.Honbou,
T.Mihara,
T.Watanabe.
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Ref.
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Bioorg Med Chem Lett, 2013,
21,
7612-7623.
[DOI no: ]
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PubMed id
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Abstract
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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.
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