Nocathiacin I analogues: synthesis, in vitro and in vivo biological activity of novel semi-synthetic thiazolyl peptide antibiotics

The synthesis and antibacterial activity of nocathiacin I analogues is described. Several nocathiacin I analogues ( 4– 35) were synthesized and evaluated for their antibacterial activity. Most of these semi-synthetic analogues retained very good in vitro and in vivo antibacterial activity of 1.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-11, Vol.14 (22), p.5573-5577
Main Authors: Naidu, B. Narasimhulu, Sorenson, Margaret E., Zhang, Yunhui, Kim, Oak K., Matiskella, John D., Wichtowski, John A., Connolly, Timothy P., Li, Wenying, Lam, Kin S., Bronson, Joanne J., Pucci, Michael J., Clark, Junius M., Ueda, Yasutsugu
Format: Article
Language:English
Subjects:
Amines - chemical synthesis
Amines - chemistry
Amines - pharmacology
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - pharmacology
Antibacterial activity
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Conjugate addition
Enterococcus faecalis - drug effects
Enterococcus faecalis - growth & development
Frozen water
General aspects
Medical sciences
Microbial Sensitivity Tests
Miscellaneous
Molecular Structure
Nocathiacins
Peptides - chemical synthesis
Peptides - pharmacology
Pharmacology. Drug treatments
Staphylococcus aureus - drug effects
Staphylococcus aureus - growth & development
Streptococcus pneumoniae - drug effects
Streptococcus pneumoniae - growth & development
Structure-Activity Relationship
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Description
Summary:The synthesis and antibacterial activity of nocathiacin I analogues is described. Several nocathiacin I analogues ( 4– 35) were synthesized and evaluated for their antibacterial activity. Most of these semi-synthetic analogues retained very good in vitro and in vivo antibacterial activity of 1.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.08.058