계명대학교 의학도서관 Repository

Discovery of a New DNA Gyrase A Inhibitor, 4-[(1-methyl-6-nitroquinolin-1-ium-4-yl)amino]-N-[4-[(1-methylpyridin-1-ium-4-yl)amino]phenyl]benzamide

Metadata Downloads
Author(s)
Incheol SeoSeong-Il SuhMin-Ho SuhWon-Ki Ba다
Keimyung Author(s)
Suh, Seong IlSuh, Min HoBaek, Won Ki
Department
Dept. of Microbiology (미생물학)
Journal Title
Journal of Bacteriology and Virology
Issued Date
2017
Volume
47
Issue
4
Keyword
Escherichia coliDNA gyraseAnti-bacterial agentsDrug discoveryZINC18057104
Abstract
Escherichia coli (E. coli) is a clinically important causative organism that can lead to urinary tract infections. Quinolone
antibiotics are among the first-line treatments for urinary tract infections. However, the frequency of resistance to quinolone
in E. coli has been increasing. Therefore, new antimicrobial agents that can be used for treatment in lieu of quinolone
antibiotics are needed. In this study, thirty-six compounds with higher scores in a virtual screening based on the threedimensional
structure of E. coli DNA gyrase were selected for in vitro antimicrobial activity testing. An in vitro test
confirmed the antimicrobial activity of 4-[(1-methyl-6-nitroquinolin-1-ium-4-yl)amino]-N-[4-[(1-methylpyridin-1-ium-
4-yl)amino]phenyl]benzamide (ZINC18057104) against E. coli among the 36 compounds. The minimum inhibitory
concentration (MIC) of ZINC18057104 against E. coli ATCC® 25922TM was 2 μg/ml, and the MIC50 and MIC90 for the
72 quinolone-resistant E. coli clinical isolates were 4 and 64 μg/ml, respectively. ZINC18057104, which has a quinoline
structure which is similar to the quinolone antibiotics, is predicted to exhibit antimicrobial activity in quinolone-resistant
E. coli because it has different molecular interactions with the DNA gyrase than that of existing quinolone antibiotics.
Keimyung Author(s)(Kor)
서성일
서민호
백원기
Publisher
School of Medicine (의과대학)
Citation
Incheol Seo et al. (2017). Discovery of a New DNA Gyrase A Inhibitor, 4-[(1-methyl-6-nitroquinolin-1-ium-4-yl)amino]-N-[4-[(1-methylpyridin-1-ium-4-yl)amino]phenyl]benzamide. Journal of Bacteriology and Virology, 47(4), 179–188. doi: 10.4167/jbv.2017.47.4.179
Type
Article
ISSN
1598-2467
DOI
10.4167/jbv.2017.47.4.179
URI
https://kumel.medlib.dsmc.or.kr/handle/2015.oak/41193
Appears in Collections:
1. School of Medicine (의과대학) > Dept. of Microbiology (미생물학)
공개 및 라이선스
  • 공개 구분공개
파일 목록

Items in Repository are protected by copyright, with all rights reserved, unless otherwise indicated.