Synthesis and antibacterial activity of doxycycline neoglycosides

J Nat Prod. 2013 Sep 27;76(9):1627-36. doi: 10.1021/np4003096. Epub 2013 Aug 29.

Abstract

A set of 37 doxycycline neoglycosides were prepared, mediated via a C-9 alkoxyamino-glycyl-based spacer reminiscent of that of tigecycline. Subsequent in vitro antibacterial assays against representative drug-resistant Gram negative and Gram positive strains revealed a sugar-dependent activity profile and one doxycycline neoglycoside, the 2'-amino-α-D-glucoside conjugate, to rival that of the parent pharmacophore. In contrast, the representative tetracycline-susceptible strain E. coli 25922 was found to be relatively responsive to a range of doxycycline neoglycosides. This study also extends the use of aminosugars in the context of neoglycosylation via a simple two-step strategy anticipated to be broadly applicable for neoglycorandomization.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Doxycycline / analogs & derivatives*
  • Doxycycline / chemical synthesis*
  • Doxycycline / chemistry
  • Doxycycline / pharmacology*
  • Escherichia coli / drug effects
  • Escherichia coli / genetics
  • Glycosides / chemical synthesis*
  • Glycosides / chemistry
  • Glycosides / pharmacology*
  • Microbial Sensitivity Tests
  • Minocycline / analogs & derivatives
  • Minocycline / pharmacology
  • Molecular Structure
  • Stereoisomerism
  • Tigecycline

Substances

  • Anti-Bacterial Agents
  • Glycosides
  • Tigecycline
  • Minocycline
  • Doxycycline