L-aspartate of erythromycin A cyclic 11,12-carbonate, a new semisynthetic erythromycin derivative

J Antibiot (Tokyo). 1976 Sep;29(9):907-14. doi: 10.7164/antibiotics.29.907.

Abstract

Erythromycin A cyclic 11,12-carbonate, a compound with high antibacterial activity, forms with L-aspartic acid a salt possessing valuable properties as a potential chemotherapeutic agent. The L-aspartate of erythromycin A cyclic 11,12-carbonate exhibits strong anti-bacterial activity, especially against Gram-positive bacteria and shows low toxicity. The serum and the lung tissue levels of the discussed salt after a single dose administration to a rat were measured in comparison with those of erythromycin, its L-aspartate, erythromycin cyclic 11,12-carbonate and its L-glutamate. The new erythromycin derivative showed definitely superior characteristics to those of the other substances tested. The activity of the L-aspartate of erythromycin A cyclic 11,12-carbonate in chemotherapy of experimental staphylococcal infection and experimental pneumococcal bronchopneumonia in mice is superior to that of the parent carbonate and erythromycin itself.

MeSH terms

  • Animals
  • Bacteria / drug effects
  • Chemical Phenomena
  • Chemistry
  • Erythromycin / analogs & derivatives*
  • Erythromycin / metabolism
  • Erythromycin / pharmacology
  • Female
  • Intestinal Absorption
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Rats
  • Staphylococcal Infections / drug therapy
  • Streptococcal Infections / drug therapy
  • Time Factors

Substances

  • Erythromycin