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Biomolecules 2018, 8(4), 166; https://doi.org/10.3390/biom8040166

High-Throughput Screen Identifying the Thiosemicarbazone NSC319726 Compound as a Potent Antimicrobial Lead Against Resistant Strains of Escherichia coli

1
Department of Veterinary and Animal Sciences, University of Copenhagen, Stigboejlen 4, 1870 Frederiksberg C, Denmark
2
Zoetis Global Therapeutics Research, 333 Portage Street, Kalamazoo, MI 49007, USA
*
Authors to whom correspondence should be addressed.
Received: 17 October 2018 / Revised: 21 November 2018 / Accepted: 3 December 2018 / Published: 7 December 2018
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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. View Full-Text
Keywords: sulfonamide resistance; antifolate; Escherichia coli; antimicrobial lead; drug discovery; multidrug resistance sulfonamide resistance; antifolate; Escherichia coli; antimicrobial lead; drug discovery; multidrug resistance
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Sadaka, C.; Damborg, P.; Watts, J.L. High-Throughput Screen Identifying the Thiosemicarbazone NSC319726 Compound as a Potent Antimicrobial Lead Against Resistant Strains of Escherichia coli. Biomolecules 2018, 8, 166.

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