ArticleBioorganic & medicinal chemistry letters2013
Inhibitors of the aminoglycoside 6'-N-acetyltransferase type Ib [AAC(6')-Ib] identified by in silico molecular docking.
Article in Bioorganic & medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 28 citations in OpenAlex.
- Inhibiting Amikacin Resistance in Multidrug-Resistant Bacteria with Cadmium and Pyrithione.Current microbiology · 2025Review
- Restoring susceptibility to aminoglycosides: identifying small molecule inhibitors of enzymatic inactivation.RSC medicinal chemistry · 2023Review
- Inhibition of Aminoglycoside 6'-Biomedicines · 2021Article
- Zinc: Multidimensional Effects on Living Organisms.Biomedicines · 2021Review
- Aminoglycoside 6'-Antibiotics (Basel, Switzerland) · 2020Article
- Multitarget Approaches against Multiresistant Superbugs.ACS infectious diseases · 2020Review
- Antibiotic resistance and inhibition mechanism of novel aminoglycoside phosphotransferase APH(5) from B. subtilis subsp. subtilis strain RK.Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology] · 2019Article
- Identification of a small molecule inhibitor of the aminoglycoside 6'-N-acetyltransferase type Ib [AAC(6')-Ib] using mixture-based combinatorial libraries.International journal of antimicrobial agents · 2018Article
- Comprehensive review of chemical strategies for the preparation of new aminoglycosides and their biological activities.Chemical Society reviews · 2018Review
- Amikacin: Uses, Resistance, and Prospects for Inhibition.Molecules (Basel, Switzerland) · 2017Review
- Effect of solvent and protein dynamics in ligand recognition and inhibition of aminoglycoside adenyltransferase 2″-Ia.Protein science : a publication of the Protein Society · 2017Article
- Identification of an Inhibitor of the Aminoglycoside 6'-MedChemComm · 2016Article
- Synthesis and Biological Activity of Mono- and Di-N-acylated Aminoglycosides.ACS medicinal chemistry letters · 2015Article
- Inhibition of aminoglycoside 6'-N-acetyltransferase type Ib-mediated amikacin resistance in Klebsiella pneumoniae by zinc and copper pyrithione.Antimicrobial agents and chemotherapy · 2015Article
- Inhibition of aminoglycoside acetyltransferase resistance enzymes by metal salts.Antimicrobial agents and chemotherapy · 2015Article
- Inhibition of aminoglycoside 6'-N-acetyltransferase type Ib by zinc: reversal of amikacin resistance in Acinetobacter baumannii and Escherichia coli by a zinc ionophore.Antimicrobial agents and chemotherapy · 2014Article
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6 authors at 1 institution in 1 country.
Funding
Abstract
AAC(6')-Ib is an important aminoglycoside resistance enzyme to target with enzymatic inhibitors. An in silico screening approach was used to identify potential inhibitors from the ChemBridge library. Several compounds were identified, of which two of them, 4-[(2-{[1-(3-methylphenyl)-4,6-dioxo-2-thioxotetrahydro-5(2H)-pyrimidinylidene]methyl}phenoxy)methyl]benzoic acid and 2-{5-[(4,6-dioxo-1,3-diphenyl-2-thioxotetrahydro-5(2H)-pyrimidinylidene)methyl]-2-furyl}benzoic acid, showed micromolar activity in inhibiting acetylation of kanamycin A. These compounds are predicted to bind the aminoglycoside binding site of AAC(6')-Ib and exhibited competitive inhibition against kanamycin A.
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