ArticleInternational journal of antimicrobial agents2018
Identification of a small molecule inhibitor of the aminoglycoside 6'-N-acetyltransferase type Ib [AAC(6')-Ib] using mixture-based combinatorial libraries.
Article in International journal of antimicrobial agents, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 22 citations in OpenAlex.
- Inhibiting Amikacin Resistance in Multidrug-Resistant Bacteria with Cadmium and Pyrithione.Current microbiology · 2025Review
- Plant-Derived Natural Products for the Treatment of Bacterial Infections.Handbook of experimental pharmacology · 2025Review
- Structure-Activity Relationship of Pyrrolidine Pentamine Derivatives as Inhibitors of the Aminoglycoside 6'-Antibiotics (Basel, Switzerland) · 2024Article
- Restoring susceptibility to aminoglycosides: identifying small molecule inhibitors of enzymatic inactivation.RSC medicinal chemistry · 2023Review
- The VirtuousAntibiotics (Basel, Switzerland) · 2023Review
- Inhibition of Enzymatic Acetylation-Mediated Resistance to Plazomicin by Silver Ions.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Discovery and development of inhibitors of acetyltransferase Eis to combat Mycobacterium tuberculosis.Methods in enzymology · 2023Article
- Amikacin in combination with zinc pyrithione prevents growth of a multidrug-resistant carbapenem-resistant Klebsiella pneumoniae isolate.International journal of antimicrobial agents · 2021Article
- Inhibition of Aminoglycoside 6'-Biomedicines · 2021Article
- Zinc: Multidimensional Effects on Living Organisms.Biomedicines · 2021Review
- Aminoglycoside 6'-Antibiotics (Basel, Switzerland) · 2020Article
- Galleria mellonella as a consolidated in vivo model hosts: New developments in antibacterial strategies and novel drug testing.Virulence · 2019Review
- SmallFrontiers in microbiology · 2019Article
- Restoration of susceptibility to amikacin by 8-hydroxyquinoline analogs complexed to zinc.PloS one · 2019Article
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Authors and funding
13 authors at 3 institutions in 1 country.
Funding
Abstract
The aminoglycoside, 6'-N-acetyltransferase type Ib [AAC(6')-Ib] is the most widely distributed enzyme among AAC(6')-I-producing Gram-negative pathogens and confers resistance to clinically relevant aminoglycosides, including amikacin. This enzyme is therefore an ideal target for enzymatic inhibitors that could overcome resistance to aminoglycosides. The search for inhibitors was carried out using mixture-based combinatorial libraries, the scaffold ranking approach, and the positional scanning strategy. A library with high inhibitory activity had pyrrolidine pentamine scaffold and was selected for further analysis. This library contained 738,192 compounds with functionalities derived from 26 different amino acids (R1, R2 and R3) and 42 different carboxylic acids (R4) in four R-group functionalities. The most active compounds all contained S-phenyl (R1 and R3) and S-hydromethyl (R2) functionalities at three locations and differed at the R4 position. The compound containing 3-phenylbutyl at R4 (compound 206) was a robust enzymatic inhibitor in vitro, in combination with amikacin it potentiated the inhibition of growth of three resistant bacteria in culture, and it improved survival when used as treatment of Galleria mellonella infected with aac(6')-Ib-harboring Klebsiella pneumoniae and Acinetobacter baumannii strains.
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