4-Aminothiazolyl analogues of GE2270 A: antibacterial lead finding

J Med Chem. 2011 Apr 14;54(7):2517-21. doi: 10.1021/jm101602q. Epub 2011 Mar 15.

Abstract

4-Aminothiazolyl analogues of the antibacterial natural product GE2270 A (1) were designed, synthesized, and evaluated for gram positive bacteria growth inhibition. The aminothiazole-based chemical template was evaluated for chemical stability, and its decomposition revealed a novel, structurally simplified, des-thiazole analogue of 1. Subsequent stabilization of the 4-aminothiazolyl functional motif was achieved and initial structure activity relationships defined.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology*
  • Bacteria / drug effects
  • Drug Discovery*
  • Drug Stability
  • Microbial Sensitivity Tests
  • Peptides, Cyclic / chemical synthesis
  • Peptides, Cyclic / chemistry*
  • Peptides, Cyclic / pharmacology*
  • Structure-Activity Relationship
  • Thiazoles / chemical synthesis
  • Thiazoles / chemistry*
  • Thiazoles / pharmacology

Substances

  • Anti-Bacterial Agents
  • Peptides, Cyclic
  • Thiazoles
  • GE 2270 A