Chemical Synthesis and Biological Screening of 2‐Aminoimidazole‐Based Bacterial and Fungal Antibiofilm Agents

Rogers, Steven A.; Bero, Joseph D.; Melander, Christian

doi:10.1002/cbic.200900617

Cited by 35 publications

(25 citation statements)

References 76 publications

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“…Replacing the unsaturated aryl appendage of 101 with a diverse array of alkyl linked amides 153,154 resulted in the discovery of several compounds with low micromolar biofilm inhibition and dispersal activity against a number of Gram-positive and Gram-negative bacterial strains (in addition to fungal anti-biofilm activity and activity against mixed species biofilms). The most active compounds possessed para -alkyl phenyl substituents and activity could again be tuned by adjusting the alkyl chain length.…”

Section: Natural Products and Natural Product Analoguesmentioning

confidence: 99%

Small molecule control of bacterial biofilms

2012

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Section: Natural Products and Natural Product Analoguesmentioning

confidence: 99%

Small molecule control of bacterial biofilms

2012

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“…[11,12] Some members of this class of compounds also possess the ability to suppress the resistance of planktonic bacteria to β-lactam antibiotics. [7] We recently reported (2-AIT) 1 (Scheme 1), which lowers the minimum inhibitory concentration (MIC) of oxacillin against an Iberian MRSA clone when co-dosed at sub-MIC levels.…”

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Potent Small‐Molecule Suppression of Oxacillin Resistance in Methicillin‐Resistant Staphylococcus aureus

2012

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The use of adjuvant molecules that have the ability to restore the susceptibility of multi-drug resistant bacteria, such as MRSA, to clinically available antibiotics is a promising alternative to the development of novel antimicrobials. We report an extremely potent small molecule that, at sub-MIC levels, lowers the MIC of oxacillin against a number of MRSA strains by up to 512-fold. Preliminary mechanistic investigations indicate that the VraSR two-component system plays a role in the activity of this compound.

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“…A variety of compounds affect bacterial as well as fungal biofilms. For example, chemically synthesized 2-aminoimidazole is known to inhibit a range of fungal and bacterial biofilms [38]. Similarly an enzymatically synthesized ester of lauroyl glucose displayed activity against both fungal and bacterial biofilms [27].…”

Section: Discussionmentioning

confidence: 99%

Disruption of Microbial Biofilms by an Extracellular Protein Isolated from Epibiotic Tropical Marine Strain of Bacillus licheniformis

et al. 2013

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BackgroundMarine epibiotic bacteria produce bioactive compounds effective against microbial biofilms. The study examines antibiofilm ability of a protein obtained from a tropical marine strain of Bacillus licheniformis D1.Methodology/Principal Findings B. licheniformis strain D1 isolated from the surface of green mussel, Perna viridis showed antimicrobial activity against pathogenic Candida albicans BH, Pseudomonas aeruginosa PAO1 and biofouling Bacillus pumilus TiO1 cultures. The antimicrobial activity was lost after treatment with trypsin and proteinase K. The protein was purified by ultrafiltration and size-exclusion chromatography. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) and matrix assisted laser desorption/ionization-time of flight (MALDI-TOF) analysis revealed the antimicrobial agent to be a 14 kDa protein designated as BL-DZ1. The protein was stable at 75°C for 30 min and over a pH range of 3.0 to 11.0. The sequence alignment of the MALDI-fingerprint showed homology with the NCBI entry for a hypothetical protein (BL00275) derived from B. licheniformis ATCC 14580 with the accession number gi52082584. The protein showed minimum inhibitory concentration (MIC) value of 1.6 µg/ml against C. albicans. Against both P. aeruginosa and B. pumilus the MIC was 3.12 µg/ml. The protein inhibited microbial growth, decreased biofilm formation and dispersed pre-formed biofilms of the representative cultures in polystyrene microtiter plates and on glass surfaces.Conclusion/SignificanceWe isolated a protein from a tropical marine strain of B. licheniformis, assigned a function to the hypothetical protein entry in the NCBI database and described its application as a potential antibiofilm agent.

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Chemical Synthesis and Biological Screening of 2‐Aminoimidazole‐Based Bacterial and Fungal Antibiofilm Agents

Cited by 35 publications

References 76 publications

Small molecule control of bacterial biofilms

Small molecule control of bacterial biofilms

Potent Small‐Molecule Suppression of Oxacillin Resistance in Methicillin‐Resistant Staphylococcus aureus

Disruption of Microbial Biofilms by an Extracellular Protein Isolated from Epibiotic Tropical Marine Strain of Bacillus licheniformis

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