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PDBsum entry 4l0l
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Penicillin binding protein/antibiotic
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PDB id
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4l0l
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References listed in PDB file
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Key reference
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Title
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Pyridone-Conjugated monobactam antibiotics with gram-Negative activity.
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Authors
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M.F.Brown,
M.J.Mitton-Fry,
J.T.Arcari,
R.Barham,
J.Casavant,
B.S.Gerstenberger,
S.Han,
J.R.Hardink,
T.M.Harris,
T.Hoang,
M.D.Huband,
M.S.Lall,
M.M.Lemmon,
C.Li,
J.Lin,
S.P.Mccurdy,
E.Mcelroy,
C.Mcpherson,
E.S.Marr,
J.P.Mueller,
L.Mullins,
A.A.Nikitenko,
M.C.Noe,
J.Penzien,
M.S.Plummer,
B.P.Schuff,
V.Shanmugasundaram,
J.T.Starr,
J.Sun,
A.Tomaras,
J.A.Young,
R.P.Zaniewski.
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Ref.
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J Med Chem, 2013,
56,
5541-5552.
[DOI no: ]
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PubMed id
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Abstract
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Herein we describe the structure-aided design and synthesis of a series of
pyridone-conjugated monobactam analogues with in vitro antibacterial activity
against clinically relevant Gram-negative species including Pseudomonas
aeruginosa , Klebsiella pneumoniae , and Escherichia coli . Rat pharmacokinetic
studies with compound 17 demonstrate low clearance and low plasma protein
binding. In addition, evidence is provided for a number of analogues suggesting
that the siderophore receptors PiuA and PirA play a role in drug uptake in P.
aeruginosa strain PAO1.
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