N⁶³-CARBOXAMIDES OF N¹⁵-ALKYL AND N¹⁵, N¹⁵-DIALKYL DERIVATIVES OF TEICOPLANIN AND DEGLUCOTEICOPLANIN

抄録

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.