EMAIL THIS PAGE TO A FRIEND

Chembiochem : a European journal of chemical biology

Identification of a novel protein synthesis inhibitor active against gram-positive bacteria.


PMID 22362659

Abstract

In an effort to identify novel antibacterial chemotypes, we performed a whole-cell screen for inhibitors of Staphylococcus aureus growth and pursued those compounds with previously uncharacterized antibacterial activity. This process resulted in the identification of a benzothiazolium salt, ABTZ-1, that displayed potent antibacterial activity against Gram-positive pathogens. Several clinically desirable qualities were demonstrated for ABTZ-1 including potent activity against multidrug-resistant clinical isolates of methicillin-resistant S. aureus (MRSA) and vancomycin-resistant enterococci (VRE), retention of this activity in human serum, and low hemolytic activity. The antibacterial activity of ABTZ-1 was attributed to its inhibition of bacterial translation, as this compound prevented the incorporation of [³⁵S]methionine into S. aureus proteins, and ABTZ-1-resistant strains were cross-resistant to known inhibitors of bacterial translation. ABTZ-1 represents a promising new class of antibacterial agents.

Related Materials

Product #

Image

Description

Molecular Formula

Add to Cart

431966
4-Formylphenylboronic acid, ≥95.0%
C7H7BO3