Quinazolinone azolyl ethanols: potential lead antimicrobial agents with dual action modes targeting methicillin-resistant Staphylococcus aureus DNA

Author:

Peng Xin-Mei1,Peng Li-Ping1,Li Shuo2,Avula Srinivasa Rao1,Kannekanti Vijaya Kumar1,Zhang Shao-Lin3,Tam Kin Yip3,Zhou Cheng-He1

Affiliation:

1. Institute of Bioorganic & Medicinal Chemistry, Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry & Chemical Engineering, Southwest University, Chongqing 400715, China

2. School of Chemical Engineering, Chongqing University of Technology, Chongqing 400054, China

3. Drug Development Core, Faculty of Health Sciences, University of Macau, Macau, China

Abstract

Aim: Due to bacterial drug resistance, a new series of quinazolinone azolyl ethanols were synthesized and evaluated. Results: In vitro antibacterial assay showed that triazolyl ethanol quinazolinone 3a was the most active compound, especially against methicillin-resistant Staphylococcus aureus (MRSA) with minimal inhibitory concentration value of 8 µg/ml, which was superior to chloromycin and comparable to norfloxacin. Molecular docking study displayed that compound 3a could interact with MRSA DNA by the formation of hydrogen bonds. Further interactions of quinazolinone 3a with MRSA DNA suggested that it could intercalate into MRSA DNA to form 3a–DNA complex. DNA cleavage properties of 3a–Cu2+ and 3a–Zn2+ complexes were confirmed by agarose gel electrophoresis experiments. Conclusion: Compound 3a should be a potential lead antibacterial molecule with dual action modes.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

全球学者库

1.学者识别学者识别

2.学术分析学术分析

3.人才评估人才评估

"全球学者库"是以全球学者为主线,采集、加工和组织学术论文而形成的新型学术文献查询和分析系统,可以对全球学者进行文献检索和人才价值评估。用户可以通过关注某些学科领域的顶尖人物而持续追踪该领域的学科进展和研究前沿。经过近期的数据扩容,当前全球学者库共收录了国内外主流学术期刊6万余种,收集的期刊论文及会议论文总量共计约1.5亿篇,并以每天添加12000余篇中外论文的速度递增。我们也可以为用户提供个性化、定制化的学者数据。欢迎来电咨询!咨询电话:010-8811{复制后删除}0370

www.globalauthorid.com

TOP

Copyright © 2019-2023 北京同舟云网络信息技术有限公司
京公网安备11010802033243号  京ICP备18003416号-3