Syntheses, structures and antibiotic activities of LpxC inhibitors based on the diacetylene scaffold.
Publication
, Journal Article
Liang, X; Lee, C-J; Chen, X; Chung, HS; Zeng, D; Raetz, CRH; Li, Y; Zhou, P; Toone, EJ
Published in: Bioorg Med Chem
January 15, 2011
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.
Duke Scholars
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Published In
Bioorg Med Chem
DOI
EISSN
1464-3391
Publication Date
January 15, 2011
Volume
19
Issue
2
Start / End Page
852 / 860
Location
England
Related Subject Headings
- Structure-Activity Relationship
- Protein Structure, Tertiary
- Molecular Sequence Data
- Microbial Sensitivity Tests
- Medicinal & Biomolecular Chemistry
- Escherichia coli Proteins
- Escherichia coli
- Enzyme Inhibitors
- Computer Simulation
- Binding Sites
Citation
APA
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ICMJE
MLA
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Liang, X., Lee, C.-J., Chen, X., Chung, H. S., Zeng, D., Raetz, C. R. H., … Toone, E. J. (2011). Syntheses, structures and antibiotic activities of LpxC inhibitors based on the diacetylene scaffold. Bioorg Med Chem, 19(2), 852–860. https://doi.org/10.1016/j.bmc.2010.12.017
Liang, Xiaofei, Chul-Jin Lee, Xin Chen, Hak Suk Chung, Daina Zeng, Christian R. H. Raetz, Yaoxian Li, Pei Zhou, and Eric J. Toone. “Syntheses, structures and antibiotic activities of LpxC inhibitors based on the diacetylene scaffold.” Bioorg Med Chem 19, no. 2 (January 15, 2011): 852–60. https://doi.org/10.1016/j.bmc.2010.12.017.
Liang X, Lee C-J, Chen X, Chung HS, Zeng D, Raetz CRH, et al. Syntheses, structures and antibiotic activities of LpxC inhibitors based on the diacetylene scaffold. Bioorg Med Chem. 2011 Jan 15;19(2):852–60.
Liang, Xiaofei, et al. “Syntheses, structures and antibiotic activities of LpxC inhibitors based on the diacetylene scaffold.” Bioorg Med Chem, vol. 19, no. 2, Jan. 2011, pp. 852–60. Pubmed, doi:10.1016/j.bmc.2010.12.017.
Liang X, Lee C-J, Chen X, Chung HS, Zeng D, Raetz CRH, Li Y, Zhou P, Toone EJ. Syntheses, structures and antibiotic activities of LpxC inhibitors based on the diacetylene scaffold. Bioorg Med Chem. 2011 Jan 15;19(2):852–860.
Published In
Bioorg Med Chem
DOI
EISSN
1464-3391
Publication Date
January 15, 2011
Volume
19
Issue
2
Start / End Page
852 / 860
Location
England
Related Subject Headings
- Structure-Activity Relationship
- Protein Structure, Tertiary
- Molecular Sequence Data
- Microbial Sensitivity Tests
- Medicinal & Biomolecular Chemistry
- Escherichia coli Proteins
- Escherichia coli
- Enzyme Inhibitors
- Computer Simulation
- Binding Sites