"Glycylcyclines". 3. 9-Aminodoxycyclinecarboxamides

J Med Chem. 1994 Sep 30;37(20):3205-11. doi: 10.1021/jm00046a003.

Abstract

A series of 9-(acylamino)doxycycline derivatives has been prepared. These analogs exhibit good activity against both tetracycline sensitive and tetracycline resistant Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria that are encoded with the efflux and ribosomal resistance gene factors. N,N-Dialkylglycylamido derivatives possessed the highest activity. Replacement of glycine moiety with other amino acids did not further enhance the activity.

MeSH terms

  • Doxycycline / analogs & derivatives*
  • Doxycycline / chemistry
  • Doxycycline / pharmacology
  • Escherichia coli / drug effects*
  • Glycine / chemistry
  • Molecular Structure
  • Staphylococcus aureus / drug effects*
  • Structure-Activity Relationship
  • Tetracycline Resistance

Substances

  • Doxycycline
  • Glycine