Works (12)

Updated: July 5th, 2023 21:21

2012 journal article

Foliar-Applied Small Molecule that Suppresses Biofilm Formation and Enhances Control of Copper-Resistant Xanthomonas euvesicatoria on Pepper

PLANT DISEASE, 96(11), 1638–1644.

By: R. Worthington, S. Rogers*, R. Huigens*, C. Melander* & D. Ritchie n

TL;DR: A small molecule additive, a member of the 2-aminoimidazole (2AI) group that is an analogue of the marine sponge natural product oroidin that suppresses resistance of Xanthomonas euvesicatoria to copper and decreases biofilm formation in an in vitro system is reported. (via Semantic Scholar)
UN Sustainable Development Goal Categories
14. Life Below Water (OpenAlex)
Source: Web Of Science
Added: August 6, 2018

2011 journal article

Synthesis and biological activity of 2-aminoimidazole triazoles accessed by Suzuki-Miyaura cross-coupling

ORGANIC & BIOMOLECULAR CHEMISTRY, 9(8), 3041–3049.

By: S. Reyes n, R. Huigens n, Z. Su n, M. Simon n & C. Melander n

MeSH headings : Acinetobacter baumannii / drug effects; Acinetobacter baumannii / physiology; Biofilms; Imidazoles / chemistry; Methicillin-Resistant Staphylococcus aureus / drug effects; Methicillin-Resistant Staphylococcus aureus / physiology; Molecular Structure; Triazoles / chemical synthesis; Triazoles / pharmacology
TL;DR: A pilot library of 2-aminoimidazole triazoles (2-AITs) was synthesized and assayed against Acinetobacter baumannii and methicillin-resistant Staphylococus aureus and they are found to possess biofilm inhibition capabilities at low micromolar concentrations. (via Semantic Scholar)
UN Sustainable Development Goal Categories
Source: Web Of Science
Added: August 6, 2018

2010 journal article

Modulating the development of E. coli biofilms with 2-aminoimidazoles

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 20(21), 6310–6312.

By: C. Reed n, R. Huigens n, S. Rogers n & C. Melander n

author keywords: 2-Aminoimidazoles; E. coli; Biofilms
MeSH headings : Acinetobacter baumannii / drug effects; Acinetobacter baumannii / growth & development; Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Drug Design; Escherichia coli / drug effects; Escherichia coli / growth & development; Hemolysis / drug effects; Humans; Imidazoles / chemical synthesis; Imidazoles / pharmacology; In Vitro Techniques; Structure-Activity Relationship
TL;DR: The synthesis of a 20 member 2-aminoimidazole/triazole pilot library is reported, with the best inhibitor inhibiting biofilm development with an IC(50) of 13μM. (via Semantic Scholar)
UN Sustainable Development Goal Categories
Source: Web Of Science
Added: August 6, 2018

2010 journal article

Synergistic Effects between Conventional Antibiotics and 2-Aminoimidazole-Derived Antibiofilm Agents

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 54(5), 2112–2118.

By: S. Rogers n, R. Huigens n, J. Cavanagh n & C. Melander n

MeSH headings : Acinetobacter baumannii / drug effects; Anti-Bacterial Agents / pharmacology; Bacteria / drug effects; Biofilms / drug effects; Calcium Chloride / pharmacology; Chlorides / pharmacology; Colistin / pharmacology; Drug Resistance, Bacterial; Drug Resistance, Multiple; Drug Synergism; Enterococcus faecium / drug effects; Erythrocytes / drug effects; Escherichia coli / drug effects; Humans; Imidazoles / chemistry; Imidazoles / pharmacology; Magnesium / pharmacology; Manganese Compounds / pharmacology; Methicillin-Resistant Staphylococcus aureus / drug effects; Novobiocin / pharmacology; Staphylococcus epidermidis / drug effects; Tobramycin / pharmacology; Triazoles / pharmacology
TL;DR: The synergistic effect between a 2-aminoimidazole/triazole conjugate and antibiotics toward dispersing preestablished biofilms, culminating with a 3-orders-of-magnitude increase of biofilm dispersion toward Staphylococcus aureus biofilmms is reported. (via Semantic Scholar)
Source: Web Of Science
Added: August 6, 2018

2009 journal article

A 2-Aminobenzimidazole That Inhibits and Disperses Gram-Positive Biofilms through a Zinc-Dependent Mechanism

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 131(29), 9868-+.

By: S. Rogers n, R. Huigens n & C. Melander n

MeSH headings : Benzimidazoles / chemical synthesis; Benzimidazoles / chemistry; Benzimidazoles / pharmacology; Biofilms / drug effects; Biofilms / growth & development; Dose-Response Relationship, Drug; Gram-Positive Bacteria / drug effects; Magnetic Resonance Spectroscopy; Molecular Structure; Structure-Activity Relationship; Zinc / chemistry; Zinc / pharmacology
TL;DR: Mechanistic studies showed that the activity of a lead 2-aminobenzimidazole is Zn(II)-dependent, potentially via a direct zinc-chelating mechanism. (via Semantic Scholar)
UN Sustainable Development Goal Categories
Source: Web Of Science
Added: August 6, 2018

2009 journal article

Evaluation of dihydrooroidin as an antifouling additive in marine paint

INTERNATIONAL BIODETERIORATION & BIODEGRADATION, 63(4), 529–532.

By: C. Melander n, P. Moeller*, T. Ballard n, J. Richards n, R. Huigens n & J. Cavanagh n

author keywords: Antifouling; Biofilms; Natural products
TL;DR: Dihydrooroidin (DHO) is presented as an effective paint-based, non-cytotoxic, antifouling agent against marine biofouling processes in a marine mesocosm. (via Semantic Scholar)
UN Sustainable Development Goal Categories
14. Life Below Water (OpenAlex)
Source: Web Of Science
Added: August 6, 2018

2009 journal article

Inhibition of Acinetobacter baumannii, Staphylococcus aureus and Pseudomonas aeruginosa biofilm formation with a class of TAGE-triazole conjugates

ORGANIC & BIOMOLECULAR CHEMISTRY, 7(4), 794–802.

By: R. Huigens n, S. Rogers n, A. Steinhauer n & C. Melander n

MeSH headings : Acinetobacter baumannii / drug effects; Anti-Bacterial Agents / chemical synthesis; Biofilms / drug effects; Imidazoles / chemistry; Pseudomonas aeruginosa / drug effects; Small Molecule Libraries / chemical synthesis; Staphylococcus aureus / drug effects; Triazoles / chemical synthesis
TL;DR: A chemically diverse library of TAGE-triazole conjugates synthesized utilizing click chemistry on the TAGE scaffold demonstrated the most potent inhibitory effect against Staphylococcus aureus biofilm formation that has been displayed by any 2-aminoimidazole derivative. (via Semantic Scholar)
Source: Web Of Science
Added: August 6, 2018

2009 journal article

The chemical synthesis and antibiotic activity of a diverse library of 2-aminobenzimidazole small molecules against MRSA and multidrug-resistant A. baumannii

BIOORGANIC & MEDICINAL CHEMISTRY, 18(2), 663–674.

By: R. Huigens n, S. Reyes n, C. Reed n, C. Bunders n, S. Rogers n, A. Steinhauer n, C. Melander n

author keywords: 2-Aminobenzimidazole; Chemical library synthesis; Antibiotic; Multidrug-resistant bacteria; Staphylococcus aureus; Acinetobacter baumannii
MeSH headings : Acinetobacter baumannii / drug effects; Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Benzimidazoles / chemical synthesis; Benzimidazoles / chemistry; Benzimidazoles / pharmacology; Drug Resistance, Multiple, Bacterial; Methicillin-Resistant Staphylococcus aureus / drug effects; Microbial Sensitivity Tests; Molecular Conformation; Small Molecule Libraries; Stereoisomerism; Structure-Activity Relationship
TL;DR: These active 2-aminobenzimidazoles retain their antibiotic activity against several strains of multidrug-resistant Staphylococcus aureus and Acinetobacter baumannii when compared to susceptible strains. (via Semantic Scholar)
UN Sustainable Development Goal Categories
Source: Web Of Science
Added: August 6, 2018

2008 journal article

Control of bacterial biofilms with marine alkaloid derivatives

MOLECULAR BIOSYSTEMS, 4(6), 614–621.

By: R. Huigens n, L. Ma, C. Gambino n, P. Moeller, A. Basso n, J. Cavanagh n, D. Wozniak*, C. Melander n

MeSH headings : Acinetobacter baumannii / drug effects; Acylation; Alkaloids / chemical synthesis; Alkaloids / chemistry; Alkaloids / pharmacology; Animals; Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Biofilms / growth & development; Bordetella bronchiseptica / drug effects; Cell Line; Dose-Response Relationship, Drug; Imidazoles / chemical synthesis; Imidazoles / chemistry; Imidazoles / pharmacology; Mice; Microbial Sensitivity Tests; Molecular Structure; Pseudomonas aeruginosa / drug effects; Rats; Staphylococcus aureus / drug effects
TL;DR: It is demonstrated that TAGE does not have selective toxicity against cells within the biofilm state, will inhibit biofilm development under flow conditions, indicating that the CV staining protocol correlates with the ability to be active under biomimetic conditions, and will disperse preformed P. aeruginosa biofilms. (via Semantic Scholar)
UN Sustainable Development Goal Categories
14. Life Below Water (OpenAlex)
Source: Web Of Science
Added: August 6, 2018

2008 journal article

Inhibition and dispersion of proteobacterial biofilms

Chemical Communications (Cambridge, England), (14), 1698–1700.

Source: NC State University Libraries
Added: August 6, 2018

2008 journal article

Synthesis and screening of an oroidin library against Pseudomonas aeruginosa biofilms

CHEMBIOCHEM, 9(8), 1267–1279.

By: J. Richards n, T. Ballard n, R. Huigens n & C. Melander n

author keywords: biological activity; drug design; medicinal chemistry; natural products; structure-activity relationships
MeSH headings : Biofilms; Cross-Linking Reagents / chemistry; Databases, Factual; Drug Design; Drug Evaluation, Preclinical; Molecular Structure; Pseudomonas aeruginosa / drug effects; Pyrroles / chemical synthesis; Pyrroles / chemistry; Pyrroles / pharmacology; Structure-Activity Relationship
TL;DR: The synthesis and determined biological activity of this unique class of compounds as inhibitors of biofilm formation that have no direct antibiotic effect are disclosed. (via Semantic Scholar)
UN Sustainable Development Goal Categories
14. Life Below Water (OpenAlex)
Source: Web Of Science
Added: August 6, 2018

2007 journal article

Inhibition of Pseudomonas aeruginosa biofilm formation with bromoageliferin analogues

Journal of the American Chemical Society, 129(22), 6966-.

By: R. Huigens, J. Richards, G. Parise, T. Ballard, W. Zeng, R. Deora, C. Melander

Source: NC State University Libraries
Added: August 6, 2018

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