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PDBsum entry 4y2b
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Hydrolase/hydrolase inhibitor
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PDB id
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4y2b
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References listed in PDB file
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Key reference
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Title
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2-(Isopropylamino)thieno[3,2-D]pyrimidin-4(3h)-One derivatives as selective phosphodiesterase 7 inhibitors with potent in vivo efficacy.
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Authors
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Y.Endo,
K.Kawai,
T.Asano,
S.Amano,
Y.Asanuma,
K.Sawada,
Y.Onodera,
N.Ueo,
N.Takahashi,
Y.Sonoda,
N.Kamei,
T.Irie.
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Ref.
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Bioorg Med Chem Lett, 2015,
25,
1910-1914.
[DOI no: ]
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PubMed id
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Abstract
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A new series of thienopyrimidinones is synthesized and evaluated as selective
phosphodiesterase 7 (PDE7) inhibitors for the treatment of inflammatory
diseases. The modification of the substituents on thienopyrimidinone revealed
that an isopropylamino group at the 2-position was favorable for aqueous
solubility. The introduction of 3-pyrrolidines at the 7-position resulted in
good solubility, highly potent activity, and good PDE7 selectivity. Among the
synthesized compounds, compound 46 exhibited the greatest inhibition of ear
edema in a phorbol ester-induced mouse model.
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