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PDBsum entry 3ch6
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Oxidoreductase
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PDB id
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3ch6
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References listed in PDB file
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Key reference
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Title
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Pyridine amides as potent and selective inhibitors of 11beta-Hydroxysteroid dehydrogenase type 1.
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Authors
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H.Wang,
Z.Ruan,
J.J.Li,
L.M.Simpkins,
R.A.Smirk,
S.C.Wu,
R.D.Hutchins,
D.S.Nirschl,
K.Van kirk,
C.B.Cooper,
J.C.Sutton,
Z.Ma,
R.Golla,
R.Seethala,
M.E.Salyan,
A.Nayeem,
S.R.Krystek,
S.Sheriff,
D.M.Camac,
P.E.Morin,
B.Carpenter,
J.A.Robl,
R.Zahler,
D.A.Gordon,
L.G.Hamann.
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Ref.
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Bioorg Med Chem Lett, 2008,
18,
3168-3172.
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PubMed id
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Abstract
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Several series of pyridine amides were identified as selective and potent
11beta-HSD1 inhibitors. The most potent inhibitors feature 2,6- or
3,5-disubstitution on the pyridine core. Various linkers (CH(2)SO(2), CH(2)S,
CH(2)O, S, O, N, bond) between the distal aryl and central pyridyl groups are
tolerated, and lipophilic amide groups are generally favored. On the distal aryl
group, a number of substitutions are well tolerated. A crystal structure was
obtained for a complex between 11beta-HSD1 and the most potent inhibitor in this
series.
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