Total Synthesis of Plusbacin A3: Depsipeptide Antibiotic Active Against Vancomycin-Resistant Bacteria.

Solid- and solution-phase synthesis of vancomycin and vancomycin analogues with activity against vancomycin-resistant bacteria.

Vancomycin, the prototypical member of the glycopeptide family of antibiotics, is a clinically used antibiotic employed against a variety of drug-resistant bacterial strains including methicillin-resistant Staphylococcus aureus (MRSA). The recent emergence of vancomycin resistance, viewed as a growing threat to public health, prompted us to initiate a program aimed at restoring the potency of t...

Synthesis of aminotrideoxybutirosin A, a chemically modified antibiotic active against butirosin-resistant bacteria.

5"-Amino-3',4'5"-trideoxybutirosin A (4) was synthesized by two routes starting from the known tri-O-acetyl-tetra-N-benzyloxycarbonyl-3",5"-O-cyclohexylidene-3',4'-di-O-mesylbutirosin A (5). Introduction of amino function at C-5" was carried out by displacement of 5"-tosyloxy group with sodium azide either before or after 3',4'-deoxygenation. Compound 4 shows outstanding activities against stra...

Synthesis of 3"-epi-dihydrostreptomycin active against resistant bacteria.

Nitrofurantoin is active against vancomycin-resistant enterococci.

The activity of nitrofurantoin was tested against 300 isolates of Enterococcus faecium, Enterococcus faecalis, and Enterococcus gallinarum. No isolates tested were resistant to nitrofurantoin (MIC, >/=128 microg/ml), including vancomycin-resistant E. faecium isolates with vanA- and vanB-positive genotypes and vancomycin-resistant E. gallinarum isolates. We conclude that nitrofurantoin may provi...

Synthesis of rigidly-linked vancomycin dimers and their in vivo efficacy against resistant bacteria.

A novel and efficient avenue for the preparation of dimeric vancomycins is described, and the dimers exhibited excellent antibacterial activities in the murine infection model.