Investigating the antibacterial activity of salen/salophene metal complexes: Induction of ferroptosis as part of the mode of action

金黄色葡萄球菌 化学 环丙沙星 大肠杆菌 细菌 抗菌活性 微生物学 四环素 铜绿假单胞菌 抗菌剂 席夫碱 革兰氏阳性菌 行动方式 抗生素 金属 生物化学 立体化学 生物 有机化学 基因 遗传学
作者
Daniel Baecker,Özcan Sesli,Ludwig Knabl,Silke Huber,Dorothea Orth‐Höller,Ronald Gust
出处
期刊:European journal of medicinal chemistry [Elsevier BV]
卷期号:209: 112907-112907 被引量:38
标识
DOI:10.1016/j.ejmech.2020.112907
摘要

The continuous increase of resistant bacteria including Staphylococcus aureus and its methicillin-resistant phenotype (MRSA) is currently one of the major challenges in medicine. Therefore, the discovery of novel lead structures for the design of drugs to fight against infections caused by these bacteria is urgently needed. In this structure-activity relationship study, metal-based drugs were investigated for the treatment of resistant pathogens. The selected Ni(II), Cu(II), Zn(II), Mn(III), and Fe(II/III) complexes differ in their salen- and salophene-type Schiff base ligands. The in vitro activity was evaluated using gram-positive (S. aureus and MRSA) and gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa). Especially the iron(III) complexes displayed promising antimicrobial effects against gram-positive bacteria, with MIC90 values ranging from 0.781 to 50 μg/mL. Among them, chlorido[(N,N′-bis(salicylidene)-1,2-phenylenediamine]iron(III) (6) showed the best MIC90 value (0.781 μg/mL = 1.93 μmol/L) against S. aureus and MRSA. Complex 6 was comparably potent as ciprofloxacin against S. aureus (0.391 μg/mL = 1.18 μmol/L) and only marginally less active than tetracycline against MRSA (0.391 μg/mL = 0.88 μmol/L). As part of the mode of action, ferroptosis was identified. Applying compound 6 (10 μg/mL), both gram-positive strains grown in PBS were killed within 20 min. This efficacy basically documents that salophene iron(III) complexes represent possible lead structures for the further development of antibacterial metal complexes.
最长约 10秒,即可获得该文献文件

科研通智能强力驱动
Strongly Powered by AbleSci AI
更新
PDF的下载单位、IP信息已删除 (2025-6-4)

科研通是完全免费的文献互助平台,具备全网最快的应助速度,最高的求助完成率。 对每一个文献求助,科研通都将尽心尽力,给求助人一个满意的交代。
实时播报
量子星尘发布了新的文献求助10
1秒前
hh完成签到,获得积分10
1秒前
所所应助Wang采纳,获得10
3秒前
付艳发布了新的文献求助10
4秒前
heure发布了新的文献求助20
4秒前
Owen应助天真皓轩采纳,获得10
4秒前
5秒前
彭彭完成签到,获得积分10
5秒前
知栀完成签到 ,获得积分10
6秒前
柔弱的千秋完成签到,获得积分20
7秒前
8秒前
四辈发布了新的文献求助10
11秒前
13秒前
跳跃的冬灵关注了科研通微信公众号
13秒前
13秒前
14秒前
14秒前
星辰大海应助宫_采纳,获得10
15秒前
吉星发布了新的文献求助10
17秒前
有爱便神经完成签到,获得积分10
17秒前
大模型应助科研通管家采纳,获得10
17秒前
在水一方应助壮观的擎采纳,获得10
17秒前
田様应助科研通管家采纳,获得10
17秒前
NexusExplorer应助科研通管家采纳,获得10
17秒前
18秒前
烟花应助科研通管家采纳,获得10
18秒前
18秒前
18秒前
18秒前
18秒前
18秒前
18秒前
天真皓轩发布了新的文献求助10
18秒前
18秒前
18秒前
18秒前
英俊的铭应助重要衬衫采纳,获得10
19秒前
科研通AI2S应助犹豫的甜瓜采纳,获得10
22秒前
xuan完成签到,获得积分10
22秒前
老实的美女完成签到,获得积分10
24秒前
高分求助中
The Mother of All Tableaux Order, Equivalence, and Geometry in the Large-scale Structure of Optimality Theory 2400
Ophthalmic Equipment Market by Devices(surgical: vitreorentinal,IOLs,OVDs,contact lens,RGP lens,backflush,diagnostic&monitoring:OCT,actorefractor,keratometer,tonometer,ophthalmoscpe,OVD), End User,Buying Criteria-Global Forecast to2029 2000
A new approach to the extrapolation of accelerated life test data 1000
Cognitive Neuroscience: The Biology of the Mind 1000
Cognitive Neuroscience: The Biology of the Mind (Sixth Edition) 1000
Optimal Transport: A Comprehensive Introduction to Modeling, Analysis, Simulation, Applications 800
Official Methods of Analysis of AOAC INTERNATIONAL 600
热门求助领域 (近24小时)
化学 材料科学 医学 生物 工程类 有机化学 生物化学 物理 内科学 纳米技术 计算机科学 化学工程 复合材料 遗传学 基因 物理化学 催化作用 冶金 细胞生物学 免疫学
热门帖子
关注 科研通微信公众号,转发送积分 3959633
求助须知:如何正确求助?哪些是违规求助? 3505879
关于积分的说明 11126688
捐赠科研通 3237840
什么是DOI,文献DOI怎么找? 1789380
邀请新用户注册赠送积分活动 871691
科研通“疑难数据库(出版商)”最低求助积分说明 802963