A Flexible Approach to 1,4-di-substituted 2-aminoimidazoles That Inhibit and Disperse Biofilms and Potentiate the Effects of β-lactams Against Multi-drug Resistant Bacteria

Overview

Journal Eur J Med Chem

Specialty Chemistry

Date 2013 Jan 29

PMID 23353733

Citations 14

Authors

Robert E Furlani

Andrew A Yeagley

Christian Melander

Affiliations

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Abstract

The pyrrole-imidazole alkaloids are a 2-aminoimidazoles containing family of natural products that possess anti-biofilm activity. A library of 1,4-di-substituted 2-aminoimidazole/triazoles (2-AITs) was synthesized, and its anti-biofilm activity as well as oxacillin resensitization efficacy toward methicillin resistant Staphylococcus aureus (MRSA) was investigated. These 2-AITs were found to inhibit biofilm formation by MRSA with low micromolar IC50 values. Additionally, the most active compound acted synergistically with oxacillin against MRSA lowering the minimum inhibitory concentration (MIC) 4-fold.

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