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PDBsum entry 3ndm
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Transferase/transferase inhibitor
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PDB id
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3ndm
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References listed in PDB file
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Key reference
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Title
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Substituted 2h-Isoquinolin-1-Ones as potent rho-Kinase inhibitors: part 3, Aryl substituted pyrrolidines.
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Authors
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T.Bosanac,
E.R.Hickey,
J.Ginn,
M.Kashem,
S.Kerr,
S.Kugler,
X.Li,
A.Olague,
S.Schlyer,
E.R.Young.
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Ref.
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Bioorg Med Chem Lett, 2010,
20,
3746-3749.
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PubMed id
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Abstract
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The discovery and SAR of a series of beta-aryl substituted pyrrolidine
2H-isoquinolin-1-one inhibitors of Rho-kinase (ROCK) derived from 2 is herein
described. SAR studies have shown that aryl groups in the beta-position are
optimal for potency. Our efforts focused on improving the ROCK potency of this
isoquinolone class of inhibitors which led to the identification of pyrrolidine
32 which demonstrated a 10-fold improvement in aortic ring (AR) potency over 2.
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Secondary reference #1
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Title
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Substituted 2h-Isoquinolin-1-Ones as potent rho-Kinase inhibitors: part 2, Optimization for blood pressure reduction in spontaneously hypertensive rats.
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Authors
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J.D.Ginn,
T.Bosanac,
R.Chen,
C.Cywin,
E.Hickey,
M.Kashem,
S.Kerr,
S.Kugler,
X.Li,
A.Prokopowicz,
S.Schlyer,
J.D.Smith,
M.R.Turner,
F.Wu,
E.R.Young.
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Ref.
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Bioorg Med Chem Lett, 2010,
20,
5153-5156.
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PubMed id
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