Design and Synthesis of Small Molecules as Potent Staphylococcus aureus Sortase A Inhibitors

Antibiotics (Basel). 2020 Oct 16;9(10):706. doi: 10.3390/antibiotics9100706.

Abstract

The widespread and uncontrollable emergence of antibiotic-resistant bacteria, especially methicillin-resistant Staphylococcus aureus, has promoted a wave of efforts to discover a new generation of antibiotics that prevent or treat bacterial infections neither as bactericides nor bacteriostats. Due to its crucial role in virulence and its nonessentiality in bacterial survival, sortase A has been considered as a great target for new antibiotics. Sortase A inhibitors have emerged as promising alternative antivirulence agents against bacteria. Herein, the structural and preparative aspects of some small synthetic organic compounds that block the pathogenic action of sortase A have been described.

Keywords: Staphylococcus aureus; drug resistant; small organic molecule; sortase A; sortase A inhibitor; synthetic chemistry.

Publication types

  • Review