Boron-containing peptidomimetics--a novel class of selective anti-tubercular drugs

Chem Biol Drug Des. 2013 Mar;81(3):408-13. doi: 10.1111/cbdd.12091. Epub 2012 Dec 26.

Abstract

Medical treatment for tuberculosis is complicated nowadays by the appearance of new multiresistant strains, and therefore, new antibiotics are in great need. Here, we report the synthesis and in vitro testing of a new class of highly selective antimicrobial boron-containing peptidomimetics with compounds exhibiting activity against Mycobacterium tuberculosis at ≤5 μg/mL. The new approach developed makes it possible to synthesize variously substituted β-aminoboronic acids and their derivatives with a high level of diastereoselectivity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antitubercular Agents / chemical synthesis
  • Antitubercular Agents / chemistry*
  • Antitubercular Agents / pharmacology
  • Boron / chemistry*
  • Boronic Acids / chemical synthesis
  • Boronic Acids / chemistry
  • Boronic Acids / pharmacology
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects
  • Peptidomimetics*

Substances

  • Antitubercular Agents
  • Boronic Acids
  • Peptidomimetics
  • Boron