High-throughput screen identifying the thiosemicarbazone NSC319726 compound as a potent antimicrobial lead against resistant strains of Escherichia coli

Carmen Sadaka; Peter Damborg; Jeffrey L. Watts

doi:10.3390/biom8040166

High-throughput screen identifying the thiosemicarbazone NSC319726 compound as a potent antimicrobial lead against resistant strains of Escherichia coli

Carmen Sadaka^*, Peter Damborg, Jeffrey L. Watts

^*Corresponding author af dette arbejde

1 Citationer (Scopus)

31 Downloads (Pure)

Abstract

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.

Originalsprog	Engelsk
Artikelnummer	166
Tidsskrift	Biomolecules
Vol/bind	8
Udgave nummer	4
ISSN	2218-273X
DOI	https://doi.org/10.3390/biom8040166
Status	Udgivet - 2018

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10.3390/biom8040166Licens: CC BY

High-Throughput Screen Identifying the Thiosemicarbazone NSC319726 Compound as a Potent Antimicrobial Lead Against Resistant Strains of Escherichia coliForlagets udgivne version, 386 KBLicens: CC BY

Citationsformater

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abstract = "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.",

keywords = "Antifolate, Antimicrobial lead, Drug discovery, Escherichia coli, Multidrug resistance, Sulfonamide resistance",

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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

SN - 2218-273X

VL - 8

JO - Biomolecules

JF - Biomolecules

IS - 4

M1 - 166

ER -

High-throughput screen identifying the thiosemicarbazone NSC319726 compound as a potent antimicrobial lead against resistant strains of Escherichia coli

Abstract

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