N63-carboxamides of N15-alkyl and N15, N15-dialkyl derivatives of teicoplanin and deglucoteicoplanin.
- 1 January 1993
- journal article
- Published by Japan Antibiotics Research Association in The Journal of Antibiotics
- Vol. 46 (4) , 668-675
- https://doi.org/10.7164/antibiotics.46.668
Abstract
The synthesis and biological properties of a series of N63-carboxamides of 15-N-alkylated derivatives of teicoplanin A2 (CTA) and its aglycone (TD) are described. Among the compounds, those carrying hydrophilic groups or ionizable amino functions on the N15-alkyl chain are more soluble in water than parent N15-methylated or unmodified amides. Selected compounds were more active in vitro than CTA or TD, and a few of them were also slightly more efficacious in vivo than the parent antibiotics in streptococcal septicemia in the mouse. Their degree of activity varied with the structure and length of the N15-alkyl chains.Keywords
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