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 for this work

1 Citation (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.

Original language	English
Article number	166
Journal	Biomolecules
Volume	8
Issue number	4
ISSN	2218-273X
DOIs	https://doi.org/10.3390/biom8040166
Publication status	Published - 2018

Keywords

Antifolate
Antimicrobial lead
Drug discovery
Escherichia coli
Multidrug resistance
Sulfonamide resistance

Access to Document

10.3390/biom8040166Licence: CC BY

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

Cite this

@article{2bbc05e0c6154cb39929964802b96dea,

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

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",

author = "Carmen Sadaka and Peter Damborg and Watts, {Jeffrey L.}",

year = "2018",

doi = "10.3390/biom8040166",

language = "English",

volume = "8",

journal = "Biomolecules",

issn = "2218-273X",

publisher = "MDPI",

number = "4",

}

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

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

Keywords

Access to Document

Fingerprint

Cite this