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
Language
- eng
Conference Location
- England