Abstract
A new pseudo-disaccharide NB23 with a 3',4'-methylidene protection was designed and its properties were evaluated in comparison to other two structurally related pseudo-disaccharides. The basicity of the 2'-amine was found to be well correlated to acute toxicity data in mice: the increase in the basicity is associated with the toxicity increase. Based on these data, a new pseudo-trisaccharide NB45 was constructed. NB45 exhibited significant antibacterial activity while at the same time retained low acute toxicity.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Amines / chemistry*
-
Aminoglycosides / chemical synthesis
-
Aminoglycosides / pharmacology
-
Aminoglycosides / toxicity*
-
Animals
-
Anti-Bacterial Agents / chemical synthesis
-
Anti-Bacterial Agents / pharmacology
-
Anti-Bacterial Agents / toxicity*
-
Disaccharides / chemistry
-
Disaccharides / pharmacology
-
Disaccharides / toxicity*
-
Magnetic Resonance Spectroscopy
-
Male
-
Mice
-
Mice, Inbred ICR
-
Microbial Sensitivity Tests
-
Pseudomonas aeruginosa / drug effects*
-
Pseudomonas aeruginosa / growth & development
-
Structure-Activity Relationship
-
Toxicity Tests, Acute
-
Trisaccharides / chemistry
-
Trisaccharides / pharmacology
-
Trisaccharides / toxicity*
Substances
-
Amines
-
Aminoglycosides
-
Anti-Bacterial Agents
-
Disaccharides
-
Trisaccharides