Pyrimidinone antibiotics--heterocyclic analogues with improved antibacterial spectrum

Bioorg Med Chem Lett. 2003 Aug 18;13(16):2641-5. doi: 10.1016/s0960-894x(03)00578-x.

Abstract

We report the synthesis and pharmacological evaluation of new derivatives of the natural dipeptide antibiotic TAN 1057 A,B containing heterocycles either in the beta-amino acid side chain or as mimics of the urea function. In the course of this program, we identified novel analogues that display activity towards a broader panel of Gram-positive bacteriae.

Publication types

  • Comparative Study

MeSH terms

  • Amino Acids / chemistry
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Dipeptides / chemical synthesis*
  • Dipeptides / pharmacology
  • Gram-Positive Bacteria / drug effects
  • Heterocyclic Compounds / chemical synthesis*
  • Heterocyclic Compounds / pharmacology
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Pyrimidinones / chemical synthesis*
  • Pyrimidinones / pharmacology
  • Stereoisomerism
  • Urea / chemistry

Substances

  • Amino Acids
  • Anti-Bacterial Agents
  • Dipeptides
  • Heterocyclic Compounds
  • Pyrimidinones
  • TAN 1057A
  • TAN 1057B
  • Urea