Format

Send to

Choose Destination
J Antibiot (Tokyo). 1998 Jun;51(6):560-9.

Novel glycopeptide antibiotics: N-alkylated derivatives active against vancomycin-resistant enterococci.

Author information

1
Infectious Diseases Research, Lilly Research Laboratories, Eli Lilly & Co., Indianapolis, IN 46285, USA.

Abstract

LY264826 (A82846B) is a naturally-occurring glycopeptide antibiotic, differing from vancomycin in the stereochemistry of the amino-sugar of the disaccharide function, and the presence of a third sugar attached at the benzylic position of amino acid residue 6. Despite these seemingly subtle differences, LY264826 is approximately 10 times more active than vancomycin against the enterococci. In the pursuit of new antibiotics active against multiresistant Gram-positive organisms, an extensive side chain SAR was developed focusing on the reductive alkylation of LY264826 at the amino function of the disaccharide moiety. A new series of derivatives having varying degrees of structural diversity in the side chain (e.g. varying lengths and degrees of rigidity) was found to have potent activity against vancomycin-resistant enterococci (MIC's < 1.0 microgram/ml) as well as activity against staphylococci and streptococci as good or better than vancomycin.

PMID:
9711219
DOI:
10.7164/antibiotics.51.560
[Indexed for MEDLINE]
Free full text

Supplemental Content

Full text links

Icon for J-STAGE, Japan Science and Technology Information Aggregator, Electronic
Loading ...
Support Center