Dimeric benzoboroxoles for targeted activity against Mycobacterium tuberculosis

Org Biomol Chem. 2019 Nov 6;17(43):9524-9528. doi: 10.1039/c9ob02222h.

Abstract

Dimeric benzoboroxoles that are covalently linked by a short scaffold enhance selective anti-tubercular activity. These multimeric benzoboroxole compounds are capable of engaging the specific extracellular Mycobacterium tuberculosis glycans, do not lead to the evolution of resistance and bypass the need to cross the impermeable mycobacterial cell envelope barrier.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • A549 Cells
  • Antitubercular Agents / chemical synthesis
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology*
  • Boronic Acids / chemical synthesis
  • Boronic Acids / chemistry
  • Boronic Acids / pharmacology*
  • Dimerization
  • Erythrocytes
  • Humans
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Mycobacterium tuberculosis / drug effects*

Substances

  • Antitubercular Agents
  • Boronic Acids
  • benzeneboronic acid