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

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • Liang, X; Lee, C-J; Chen, X; Chung, HS; Zeng, D; Raetz, CRH; Li, Y; Zhou, P; Toone, EJ

Published Date

  • January 15, 2011

Published In

Volume / Issue

  • 19 / 2

Start / End Page

  • 852 - 860

PubMed ID

  • 21194954

Pubmed Central ID

  • PMC3035996

Electronic International Standard Serial Number (EISSN)

  • 1464-3391

Digital Object Identifier (DOI)

  • 10.1016/j.bmc.2010.12.017


  • eng

Conference Location

  • England