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PDBsum entry 3ps2
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Hydrolase/antibiotic
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PDB id
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3ps2
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References listed in PDB file
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Key reference
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Title
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Syntheses, Structures and antibiotic activities of lpxc inhibitors based on the diacetylene scaffold.
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Authors
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X.Liang,
C.J.Lee,
X.Chen,
H.S.Chung,
D.Zeng,
C.R.Raetz,
Y.Li,
P.Zhou,
E.J.Toone.
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Ref.
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Bioorg Med Chem Lett, 2011,
19,
852-860.
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PubMed id
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Abstract
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Compounds inhibiting LpxC in the lipid A biosynthetic pathway are promising
leads for novel antibiotics against multidrug-resistant Gram-negative pathogens.
We report the syntheses and structural and biochemical characterizations of LpxC
inhibitors based on a diphenyl-diacetylene (1,4-diphenyl-1,3-butadiyne)
threonyl-hydroxamate scaffold. These studies provide a molecular interpretation
for the differential antibiotic activities of compounds with a substituted
distal phenyl ring as well as the absolute stereochemical requirement at the C2,
but not C3, position of the threonyl group.
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