Phosphonopeptides as Antibacterial Agents: Alaphosphin and Related Phosphonopeptides

Phosphonopeptides as antibacterial agents: mechanism of action of alaphosphin.

The novel antibacterial peptide mimetic alaphosphin (l-alanyl-l-1-aminoethylphosphonic acid) selectively inhibited peptidoglycan biosynthesis in both gram-negative and gram-positive bacteria. It induced accumulation of uridine diphosphate-N-acetyl-muramyl-tripeptide in gram-positive organisms and significantly reduced the intracellular pool levels of d-alanine. Alaphosphin was actively transpor...

Antibacterial activity and mechanism of action of phosphonopeptides based on aminomethylphosphonic acid.

Phosphonopeptides based on aminomethylphosphonic acid as the C-terminal residue linked to L-amino acids possessed antibacterial activity in vitro and in vivo. Analogs in this series were generally less potent than corresponding compounds based on L-1-aminoethylphosphonic acid such as alafosfalin (L-alanyl-L-1-aminoethylphosphonic acid). Significant differences in antibacterial spectra were obse...

The characteristics of peptide uptake in Streptococcus faecalis: studies on the transport of natural peptides and antibacterial phosphonopeptides.

Transport of natural peptides and antibacterial phosphonopeptide analogues was studied in Streptococcus faecalis ATCC 9790. Competition studies, and the isolation of peptide-transport deficient mutants, indicate the presence of two peptide permeases. One is a high-rate system used by dipeptides, and to a lesser extent tripeptides; the other is a low-rate oligopeptide system. Following uptake, p...

Novel Levofloxacin Derivatives as Potent Antibacterial Agents

In this report, a new series of fluoroquinolone agents which was derived from levofloxacin was synthesized and evaluated against Gram-positive (Bacillus subtillis, Staphylococcus aureus, Staphylococcus epidermidis and Micrococcus luteus) and Gram-negative (Esherichio coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and Serratia marcescens) organisms. The results showed that some of the synth...

Dendrimers as Antibacterial Agents