Synthesis, in vitro, and in vivo antibacterial activity of nocathiacin I thiol-Michael adducts

The synthesis and antibacterial activity of nocathiacin I analogues is described. The synthesis and antibacterial activity of a series of nocathiacin I derivatives ( 4– 20) containing polar water solubilizing groups is described. Thiol-Michael adducts containing acidic polar groups have reduced anti...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-04, Vol.15 (8), p.2069-2072
Main Authors: Naidu, B. Narasimhulu, Sorenson, Margaret E., Bronson, Joanne J., Pucci, Michael J., Clark, Junius M., Ueda, Yasutsugu
Format: Article
Language:English
Subjects:
Animals
Anti-Bacterial Agents - administration & dosage
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - pharmacology
Antibacterial activity
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Female
Medical sciences
Mice
Mice, Inbred ICR
Microbial Sensitivity Tests
Nocathiacin I
Peptides - administration & dosage
Peptides - chemical synthesis
Peptides - pharmacology
Pharmacology. Drug treatments
Staphylococcal Infections - drug therapy
Staphylococcus aureus - drug effects
Staphylococcus aureus - growth & development
Sulfhydryl Compounds - chemical synthesis
Sulfhydryl Compounds - pharmacology
Thiol-Michael adducts
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Summary:The synthesis and antibacterial activity of nocathiacin I analogues is described. The synthesis and antibacterial activity of a series of nocathiacin I derivatives ( 4– 20) containing polar water solubilizing groups is described. Thiol-Michael adducts containing acidic polar groups have reduced antibacterial activity whereas those with basic polar groups have retained very good antibacterial activity.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.02.046