The discovery of biaryl acids and amides exhibiting antibacterial activity against Gram-positive bacteria

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1423-6. doi: 10.1016/j.bmcl.2004.01.026.

Abstract

Solid-phase synthetic methods for biaryl-based compounds were developed resulting in the construction of two 1000-member libraries. Numerous compounds were identified by high-throughput screening using whole cell screens to exhibit anti-microbial activity against Gram-positive bacteria. A series of biaryl compounds containing natural and unnatural amino acids were made to explore the SAR of the amino acid functionality.

MeSH terms

  • Amides / chemistry
  • Amides / pharmacology*
  • Amino Acids / chemistry
  • Amino Acids / pharmacology*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Escherichia coli / drug effects*
  • Escherichia coli / growth & development
  • Gram-Positive Bacteria / drug effects
  • Gram-Positive Bacteria / growth & development
  • Microbial Sensitivity Tests / statistics & numerical data
  • Staphylococcus aureus / drug effects*
  • Staphylococcus aureus / growth & development

Substances

  • Amides
  • Amino Acids
  • Anti-Bacterial Agents