High-throughput screen identifying the thiosemicarbazone NSC319726 compound as a potent antimicrobial lead against resistant strains of Escherichia coli
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High-throughput screen identifying the thiosemicarbazone NSC319726 compound as a potent antimicrobial lead against resistant strains of Escherichia coli. / Sadaka, Carmen; Damborg, Peter; Watts, Jeffrey L.
In: Biomolecules, Vol. 8, No. 4, 166, 2018.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - High-throughput screen identifying the thiosemicarbazone NSC319726 compound as a potent antimicrobial lead against resistant strains of Escherichia coli
AU - Sadaka, Carmen
AU - Damborg, Peter
AU - Watts, Jeffrey L.
PY - 2018
Y1 - 2018
N2 - Antibiotic discovery is vital when considering the increasing antimicrobial resistance threat. The aim of this work was to provide a high-throughput screen (HTS) assay using multidrug-resistant Escherichia coli strains to enable further research into antimicrobial lead discovery and identify novel antimicrobials. This study describes a primary HTS of a diverse library of 7884 small molecules against a susceptible E. coli strain. A secondary screening of 112 molecules against four E. coli strains with different susceptibility profiles revealed NSC319726 as a potential antimicrobial lead serving as a novel template. NSC319726 is a good candidate for an analoguing program.
AB - Antibiotic discovery is vital when considering the increasing antimicrobial resistance threat. The aim of this work was to provide a high-throughput screen (HTS) assay using multidrug-resistant Escherichia coli strains to enable further research into antimicrobial lead discovery and identify novel antimicrobials. This study describes a primary HTS of a diverse library of 7884 small molecules against a susceptible E. coli strain. A secondary screening of 112 molecules against four E. coli strains with different susceptibility profiles revealed NSC319726 as a potential antimicrobial lead serving as a novel template. NSC319726 is a good candidate for an analoguing program.
KW - Antifolate
KW - Antimicrobial lead
KW - Drug discovery
KW - Escherichia coli
KW - Multidrug resistance
KW - Sulfonamide resistance
U2 - 10.3390/biom8040166
DO - 10.3390/biom8040166
M3 - Journal article
C2 - 30544635
AN - SCOPUS:85058731442
VL - 8
JO - Biomolecules
JF - Biomolecules
SN - 2218-273X
IS - 4
M1 - 166
ER -
ID: 212860448