Synthesis, antibacterial activity and docking studies of chloroacetamide derivatives

乙酰胺 氯乙酰氯 化学 DNA旋转酶 对接(动物) 组合化学 碳-13核磁共振 大肠杆菌 立体化学 分子 抗菌活性 质子核磁共振 抗菌剂 有机化学 细菌 氯化物 生物化学 护理部 基因 生物 医学 遗传学
作者
Shahzad Murtaza,Ataf Ali Altaf,Muhammad Hamayun,Kiran Iftikhar,Muhammad Nawaz Tahir,Javaria Tariq,Khadija Faiz
出处
期刊:European Journal of Chemistry [European Journal of Chemistry]
卷期号:10 (4): 358-366 被引量:14
标识
DOI:10.5155/eurjchem.10.4.358-366.1859
摘要

Structural modification of lead compounds is a great challenge in organic synthesis. Introduction of different functional groups not only modify the structure of starting material but also improve their biological activeness. Small synthetic molecules are favored in spite of the reality that majority of drug molecules derived from natural sources, are in vogue. In the present work, acetamide derivatives were synthesized using chloroacetyl chloride. After synthesizing targeted series of acetamide derivatives these compounds were further modified using different amines including 2-aminobenzene thiol, benzyl amine, benzene 1,4-diamine, 4-amino-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one, 4-aminophenol, hydrazine and 4-amino-N-(5-methylisoxazol-3-yl)benzenesulfonamide. All of these synthesized compounds were characterized by FT-IR, 1H NMR, 13C NMR and X-ray crystallography. The compounds were assessed for their anti-bacterial activity using disc diffusion method against Staphylococcus aureus and Escherichia coli. The compounds were found to exhibit comparable activity to the standard drug used. This was further supported by molecular docking studies using bacterial DNA gyrase and Topoisomerase II targets causing bacterial death as they are major bacterial proteins known to be involved in transcription and replication process. Results proved that the compound 2b was the most efficacious antimicrobial compound among the synthesized set of compounds. To tackle the growing drug resistance acetamide based functionalities can be regarded as the active lead compounds to target different drug resistance microorganism.
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
刚刚
烟花应助李大洋采纳,获得10
1秒前
无七完成签到 ,获得积分10
1秒前
猪猪hero应助科研通管家采纳,获得10
2秒前
科研通AI6应助科研通管家采纳,获得10
2秒前
2秒前
英姑应助Brian采纳,获得10
2秒前
猪猪hero应助科研通管家采纳,获得10
2秒前
执着谷兰应助科研通管家采纳,获得10
2秒前
NexusExplorer应助科研通管家采纳,获得10
2秒前
alchol应助科研通管家采纳,获得40
2秒前
alchol应助科研通管家采纳,获得40
3秒前
小二郎应助科研通管家采纳,获得10
3秒前
猪猪hero应助科研通管家采纳,获得10
3秒前
ding应助科研通管家采纳,获得30
3秒前
猪猪hero应助科研通管家采纳,获得10
3秒前
浮游应助科研通管家采纳,获得10
3秒前
科研通AI5应助科研通管家采纳,获得10
3秒前
大模型应助科研通管家采纳,获得10
3秒前
1101592875应助科研通管家采纳,获得10
3秒前
完美世界应助科研通管家采纳,获得10
3秒前
SciGPT应助科研通管家采纳,获得10
3秒前
4秒前
加菲丰丰应助科研通管家采纳,获得10
4秒前
4秒前
斯文败类应助科研通管家采纳,获得10
4秒前
科研通AI6应助科研通管家采纳,获得10
4秒前
4秒前
今后应助科研通管家采纳,获得10
4秒前
科目三应助科研通管家采纳,获得10
4秒前
CipherSage应助科研通管家采纳,获得10
4秒前
乐乐应助科研通管家采纳,获得10
4秒前
充电宝应助科研通管家采纳,获得10
4秒前
李爱国应助科研通管家采纳,获得10
4秒前
4秒前
4秒前
LiangWQ发布了新的文献求助10
5秒前
学分完成签到 ,获得积分10
5秒前
6秒前
6秒前
高分求助中
(应助此贴封号)【重要!!请各用户(尤其是新用户)详细阅读】【科研通的精品贴汇总】 10000
计划经济时代的工厂管理与工人状况(1949-1966)——以郑州市国营工厂为例 500
Sociologies et cosmopolitisme méthodologique 400
Why America Can't Retrench (And How it Might) 400
Another look at Archaeopteryx as the oldest bird 390
创造互补优势国外有人/无人协同解析 300
The Great Psychology Delusion 300
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 纳米技术 计算机科学 内科学 化学工程 复合材料 物理化学 基因 催化作用 遗传学 冶金 电极 光电子学
热门帖子
关注 科研通微信公众号,转发送积分 4647756
求助须知:如何正确求助?哪些是违规求助? 4036972
关于积分的说明 12486439
捐赠科研通 3726420
什么是DOI,文献DOI怎么找? 2056771
邀请新用户注册赠送积分活动 1087729
科研通“疑难数据库(出版商)”最低求助积分说明 969096