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PDBsum entry 5d7c
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Isomerase/isomerase inhibitor
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PDB id
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5d7c
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References listed in PDB file
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Key reference
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Title
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Discovery of azaindole ureas as a novel class of bacterial gyrase b inhibitors.
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Authors
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J.Zhang,
Q.Yang,
J.B.Cross,
J.A.Romero,
K.M.Poutsiaka,
F.Epie,
D.Bevan,
B.Wang,
Y.Zhang,
A.Chavan,
X.Zhang,
T.Moy,
A.Daniel,
K.Nguyen,
B.Chamberlain,
N.Carter,
J.Shotwell,
J.Silverman,
C.A.Metcalf,
D.Ryan,
B.Lippa,
R.E.Dolle.
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Ref.
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J Med Chem, 2015,
58,
8503-8512.
[DOI no: ]
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PubMed id
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Abstract
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The emergence and spread of multidrug resistant bacteria are widely believed to
endanger human health. New drug targets and lead compounds exempt from
cross-resistance with existing drugs are urgently needed. We report on the
discovery of azaindole ureas as a novel class of bacterial gyrase B inhibitors
and detail the story of their evolution from a de novo design hit based on
structure-based drug design. These inhibitors show potent minimum inhibitory
concentrations against fluoroquinolone resistant MRSA and other Gram-positive
bacteria.
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