Bacterial translation inhibitors, 1-acylindazol-3-ols as anthranilic acid mimics

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6293-7. doi: 10.1016/j.bmcl.2007.08.041. Epub 2007 Aug 25.

Abstract

The discovery and initial optimization of a novel anthranilic acid derived class of antibacterial agents has been described in a recent series of papers. This paper describes the discovery of 1-acylindazol-3-ols as a novel bioisostere of an anthranilic acid. The synthesis and structure-activity relationships of the indazol bioisosteres are described herein.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Combinatorial Chemistry Techniques
  • Crystallography, X-Ray
  • Indazoles / chemical synthesis*
  • Indazoles / chemistry
  • Indazoles / pharmacology*
  • Microbial Sensitivity Tests
  • Molecular Conformation
  • Molecular Structure
  • Protein Biosynthesis / drug effects*
  • Staphylococcus aureus / drug effects*
  • Structure-Activity Relationship
  • ortho-Aminobenzoates / chemistry*

Substances

  • Anti-Bacterial Agents
  • Indazoles
  • ortho-Aminobenzoates