Activity of Benzimidazole and 1-indanone-based Molecules as Inhibitors of Escherichia coli 5'-methylthioadenosine nucleosidase (MTN)

Faculty Mentor Information

John Thurston, Kenneth Cornell, Hank Dossett, Necia Hunter

Presentation Date

7-2016

Abstract

New antibiotics that exhibit novel modes of action are urgently needed to combat the continued emergence of drug-resistant microorganisms. The enzyme 5'-methylthioadenosine nucleosidase (MTN) plays a central role in microbial metabolism and replication and has been associated with exotoxin and biofilm production and the expression of drug resistant phenotypes. Inhibition of this enzyme has been shown to both reduce the observed virulence and growth rate of several organisms, including Escherichia coli. This data suggests that drugs that target bacterial MTN may have antimicrobial applications. As part of this study we have synthesized a library of potential small molecule inhibitors (SMIs) using either the benzdimidazole or the 1-indanone functional group as a molecular scaffold. The ability of the resulting SMIs to exhibit anti-MTN activity has been explored.

Comments

Poster #Th32

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Activity of Benzimidazole and 1-indanone-based Molecules as Inhibitors of Escherichia coli 5'-methylthioadenosine nucleosidase (MTN)

New antibiotics that exhibit novel modes of action are urgently needed to combat the continued emergence of drug-resistant microorganisms. The enzyme 5'-methylthioadenosine nucleosidase (MTN) plays a central role in microbial metabolism and replication and has been associated with exotoxin and biofilm production and the expression of drug resistant phenotypes. Inhibition of this enzyme has been shown to both reduce the observed virulence and growth rate of several organisms, including Escherichia coli. This data suggests that drugs that target bacterial MTN may have antimicrobial applications. As part of this study we have synthesized a library of potential small molecule inhibitors (SMIs) using either the benzdimidazole or the 1-indanone functional group as a molecular scaffold. The ability of the resulting SMIs to exhibit anti-MTN activity has been explored.