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Ergot Alkaloid Antibacterial Activity via Novel Mechanism

Metergoline and analogues as inhibitors of Salmonella, MRSA, and S. aureus

Background

Antimicrobial resistance in Gram-positive and Gram-negative bacteria is a threat to global public health. Indeed, there is a pressing need to develop new antibiotics and adjuvants with new scaffolds and mechanisms of action (MOA). Salmonella enterica serovar Typhimurium (S. Tm) is on the WHO list of priority pathogens as a leading cause of gastroenteritis worldwide and classified as a serious antibiotic resistance threat by the U.S. Centers for Disease Control.

Technology Overview

Researchers at McMaster developed a phenotypic high-throughput screen for inhibitors of Salmonella growth within macrophages and identified metergoline as a hit. Further research on the mechanism of action has identified the compound, and potent analogues, bind an alternate binding site in DNA gyrase and represent a distinct

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