N63-CARBOXAMIDES OF N-15-ALKYL AND N15,N15-DIALKYL DERIVATIVES OF TEICOPLANIN AND DEGLUCOTEICOPLANIN

The synthesis and biological properties of a series of N63-carboxamide s of 15-N-alkylated derivatives of teicoplanin A2 (CTA) and its aglyco ne (TD) are described. Among the compounds, those carrying hydrophilic groups or ionizable amino functions on the N-15-alkyl chain are more soluble in water than parent N-15-methylated or unmodified amides. Sel ected 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 anti biotics in streptococcal septicemia in the mouse. Their degree of acti vity varied with the structure and length of the N-15-alkyl chains.