phosphoramidon and Keratitis

Topics: Animals; Bacterial Proteins; Dipeptides; Glycopeptides; Keratitis; Leucine; Metalloendopeptidases; Pseudomonas aeruginosa; Pseudomonas Infections; Rabbits; Serine Proteinase Inhibitors

Phosphoramidon (N-(alpha-L-rhamnopyranosyloxyhydroxyphosphinyl)-L-leucyl-L-trypto phan) is a powerful inhibitor of Pseudomonas aeruginosa elastase. The addition of this compound to an elastase solution injected intrastromally in rabbit eyes protected the corneas from the damage of the enzyme for a period of 12 hours. Phosphoramidon is comparable in this respect to the inhibitor 2-mercaptoacetyl-L-phenylalanyl-L-leucine, but is considerably more effective than its analog phosphoryl-L-leucyl-L-phenylalanine (P-Leu-Phe). It is suggested that the rhamnopyranosyl moiety, present in phosphoramidon but not in P-Leu-Phe, is responsible for the difference in the intracorneal activity of the two phosphoramidates. Phosphoramidon as well as the mercaptoacetyl derivative might prove beneficial in the treatment of Pseudomonas aeruginosa corneal infections.

Topics: Animals; Chemical Phenomena; Chemistry; Cornea; Dipeptides; Drug Evaluation, Preclinical; Glycopeptides; Injections; Keratitis; Pancreatic Elastase; Pseudomonas aeruginosa; Pseudomonas Infections; Rabbits