High-Throughput Screen Identifying the Thiosemicarbazone N5C319726 Compound as a Potent Antimicrobial Lead Against Resistant Strains of Escherichia coli

被引：5

作者：

Sadaka, Carmen ^{[1
]}

Damborg, Peter ^{[2
]}

Watts, Jeffrey L. ^{[2
]}

机构：

[1] Univ Copenhagen, Dept Vet & Anim Sci, Stigboejlen 4, DK-1870 Frederiksberg C, Denmark

[2] Zoetis Global Therapeut Res, 333 Portage St, Kalamazoo, MI 49007 USA

来源：

BIOMOLECULES | 2018年 / 8卷 / 04期

关键词：

sulfonamide resistance; antifolate; Escherichia coli; antimicrobial lead; drug discovery; multidrug resistance; DRUG-DISCOVERY; AGREEMENT; ANTIBIOTICS;

D O I：

10.3390/biom8040166

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页数：8