Discovery of meta-Amido Bromophenols as New Antitubercular Agents

Chem Pharm Bull (Tokyo). 2019 Apr 1;67(4):372-381. doi: 10.1248/cpb.c18-00917. Epub 2019 Jan 26.

Abstract

A series of meta-amido bromophenol derivatives were designed and synthesized. The compounds were found to potently inhibit the growth of Mycobacterium tuberculosis H37Ra. They also exhibited moderate inhibitory activity against Mycobacterium tuberculosis H37Rv and multidrug-resistant strains. The compounds did not show inhibitory activity against normal Gram-positive and Gram-negative bacteria. Moderate cytotoxicities and good metabolic stability were observed for the selected compounds. The results demonstrated meta-amido bromophenols as a new class of antitubercular agents with good potentials.

Keywords: Mycobacterium tuberculosis; antitubercular agent; meta-amido bromophenol.

MeSH terms

  • Antitubercular Agents / chemistry*
  • Drug Design
  • Drug Resistance, Multiple, Bacterial / drug effects
  • Gram-Negative Bacteria / drug effects
  • Gram-Positive Bacteria / drug effects
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects
  • Phenols / chemistry*
  • Phenols / pharmacology
  • Structure-Activity Relationship

Substances

  • Antitubercular Agents
  • Phenols
  • 3-bromophenol