Triazole-based aminoglycoside-peptide conjugates and methods...

C - Chemistry – Metallurgy – 07 – H

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C07H 19/056 (2006.01) A61K 31/7028 (2006.01) A61K 45/00 (2006.01) A61P 31/04 (2006.01) C07G 3/00 (2006.01) C07G 11/00 (2006.01) C07K 1/06 (2006.01) C07K 4/00 (2006.01) C07K 5/078 (2006.01) C07K 5/097 (2006.01) C07K 5/117 (2006.01) C07K 9/00 (2006.01)

Patent

CA 2687689

Aminoglycoside-amino acid and -peptide conjugates comprising a triazolyl linker are provided along with efficient methods of their preparation. The aminoglycoside may be an aminoglycoside antibiotic. Conjugates comprising an aminoglycoside antibiotic may exhibit antimicrobial activities against Gram-positive and/or Gram-negative strains and display significantly enhanced activity against multi-drug resistant MRSA and MRSE when compared to their unconjugated aminoglycoside antibiotic counterparts.

La présente invention concerne des conjugués aminoglycoside-acide aminé et amiglycoside-peptide qui comprennent un lieur triazolyle, ainsi que des procédés performants pour les préparer. L'aminoglycoside peut être un antibiotique aminoglycoside. Les conjugués comprenant un antibiotique aminoglycoside peuvent présenter des activités antimicrobiennes contre les souches à Gram positif et/ou à Gram négatif et affichent une activité significativement accrue contre les SARM et SERM multirésistants par rapport à leurs homologues antibiotiques aminoglycosides non conjugués.

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