Works (8)

Updated: July 23rd, 2023 19:25

2015 journal article

Membrane-Permeabilizing Activity of Reverse-Amide 2-Aminoimidazole Antibiofilm Agents Against Acinetobacter baumannii

CURRENT DRUG DELIVERY, 12(2), 223–230.

By: S. Stowe*, R. Thompson*, L. Peng*, Z. Su*, M. Blackledge*, G. Draughn, W. Coe, E. Johannes* ...

author keywords: 2-aminoimidazole; Acinetobacter baumannii; biofilm; membrane permeabilization; reverse amide; SEM
MeSH headings : Acinetobacter baumannii / drug effects; Amides / chemistry; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Cell Membrane Permeability / drug effects; Cells, Cultured; Cross Infection; Imidazoles / chemistry; Imidazoles / pharmacology; Microbial Sensitivity Tests
TL;DR: A model is proposed that describes how the structure of RA-2AI allows it to insert itself into and disrupt the fluidity of the membrane, creating an opportunity for increased molecular permeability. (via Semantic Scholar)
UN Sustainable Development Goal Categories
Source: Web Of Science
Added: August 6, 2018

2012 journal article

Identification of BfmR, a Response Regulator Involved in Biofilm Development, as a Target for a 2-Aminoimidazole-Based Antibiofilm Agent

BIOCHEMISTRY, 51(49), 9776–9778.

MeSH headings : Acinetobacter baumannii / drug effects; Acinetobacter baumannii / growth & development; Bacterial Proteins / chemistry; Bacterial Proteins / physiology; Biofilms / drug effects; Imidazoles / pharmacology; Microscopy, Confocal; Models, Molecular
TL;DR: The 2AI compound studied here represents a unique small molecule scaffold that targets bacterial response regulators and is cell permeable, while pull-down assays identified BfmR, a response regulator that is the master controller of biofilm formation, as a target for this compound. (via Semantic Scholar)
Source: Web Of Science
Added: August 6, 2018

2012 journal article

N-Substituted 2-aminoimidazole inhibitors of MRSA biofilm formation accessed through direct 1,3-bis(tert-butoxycarbonyl)guanidine cyclization

ORGANIC & BIOMOLECULAR CHEMISTRY, 11(1), 130–137.

By: A. Yeagley n, Z. Su n, K. McCullough n, R. Worthington n & C. Melander n

MeSH headings : Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Biofilms / growth & development; Cyclization; Guanidines / chemistry; Imidazoles / chemical synthesis; Imidazoles / chemistry; Imidazoles / pharmacology; Methicillin-Resistant Staphylococcus aureus / drug effects; Molecular Structure; Structure-Activity Relationship; Triazoles / chemical synthesis; Triazoles / chemistry; Triazoles / pharmacology
TL;DR: A library of N-substituted derivatives of a previously reported 2-aminoimidazole/triazole (2-AIT) biofilm modulator exhibited synergistic activity with oxacillin against planktonic MRSA and has the potential to be used as adjuvants with conventional antibiotics. (via Semantic Scholar)
UN Sustainable Development Goal Categories
Source: Web Of Science
Added: August 6, 2018

2011 journal article

A modular approach to the synthesis of 1,4,5-substituted-2-aminoimidazoles

TETRAHEDRON LETTERS, 53(10), 1204–1206.

By: Z. Su n, L. Peng n & C. Melander n

author keywords: N-H insertion; 2-Aminoimidazole; Antibiotic; Polysubstitution; Heterocycle
UN Sustainable Development Goal Categories
Source: Web Of Science
Added: August 6, 2018

2011 journal article

Evaluation of 4,5-Disubstituted-2-Aminoimidazole-Triazole Conjugates for Antibiofilm/Antibiotic Resensitization Activity Against MRSA and Acinetobacter baumannii

CHEMMEDCHEM, 6(12), 2243–2251.

By: Z. Su n, L. Peng n, R. Worthington n & C. Melander n

author keywords: aminoimidazoles; antibiotic resensitization; biofilms; MRSA; synergism
MeSH headings : Acinetobacter baumannii / drug effects; Acinetobacter baumannii / physiology; Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Imidazoles / chemistry; Methicillin-Resistant Staphylococcus aureus / drug effects; Methicillin-Resistant Staphylococcus aureus / physiology; Oxacillin / chemistry; Oxacillin / pharmacology; Structure-Activity Relationship; Triazoles / chemistry
TL;DR: This class of small molecules was found to inhibit biofilm formation by methicillin‐resistant Staphylococcus aureus (MRSA) at low‐micromolar concentrations and the ability of selected compounds to resensitize MRSA to traditional antibiotics (resensitization activity) was determined. (via Semantic Scholar)
UN Sustainable Development Goal Categories
Source: Web Of Science
Added: August 6, 2018

2011 journal article

Inhibition of Acinetobacter baumannii biofilm formation on a methacrylate polymer containing a 2-aminoimidazole subunit

Chemical Communications (Cambridge, England), 47(17), 4896–4898.

By: L. Peng, J. DeSousa, Z. Su, B. Novak, A. Nevzorov, E. Garland, C. Melander

Source: NC State University Libraries
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

A nitroenolate approach to the synthesis of 4,5-disubstituted-2-aminoimidazoles. Pilot library assembly and screening for antibiotic and antibiofilm activity

Organic & Biomolecular Chemistry, 8(12), 2814–2822.

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

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