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Bioorg Med Chem. 2011 Jan 15;19(2):852-60. doi: 10.1016/j.bmc.2010.12.017. Epub 2010 Dec 9.

Syntheses, structures and antibiotic activities of LpxC inhibitors based on the diacetylene scaffold.

Author information

1
Department of Chemistry, Jilin University, Changchun, PR China.

Abstract

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.

PMID:
21194954
PMCID:
PMC3035996
DOI:
10.1016/j.bmc.2010.12.017
[Indexed for MEDLINE]
Free PMC Article

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