The Synthesis and Antibacterial Activity of N-((1H-benzimidazol-2- yl)methyl)-2-substituted-3H- benzimidazol-5-amine Derivatives

胺气处理 化学 抗菌活性 组合化学 药物化学 有机化学 细菌 生物 遗传学
作者
Balasaheb Pathare,Tanaji N. Bansode
出处
期刊:Current Chinese chemistry journal 卷期号:03
标识
DOI:10.2174/0126660016296466240219060642
摘要

Abstract: The increasing commonality of multi-drug-resistant bacteria as well as fungi is the motive for the development of new active antimicrobial agents. Heterocyclic compounds are major contributors in medical chemistry and are also found in biomolecules like vitamins, enzymes, natural products, etc. Benzimidazole is one of the nitrogens-containing heterocyclic compounds. Derivatives of benzimidazole have been found active against various bacterial diseases. Benzimidazole derivatives containing two benzimidazole rings also showed various pharmacological activities. In view of these, we aim to synthesize a new series of benzimidazole derivatives, N-((1H-benzimidazol-2-yl)methyl)-2-substituted-3H- benzimidazol-5-amine (6a–f) by the reaction of substituted 5-aminobenzimidazol derivatives with 2-chloromethyl benzimidazole and study their predicted bioactivity and actual antibacterial activity. To confirm the structures of the synthesized compounds, spectroscopic techniques like IR, 1H NMR,13C NMR and mass spectra were used. Initially, predicted bioactivity was studied using Molinspiration software. Among the synthesized compounds (6a-f), compounds 6a, 6d, 6e, and 6f showed good predicted activity. Then all the synthesized compounds 6a–f were screened for their antibacterial activity against E. coli (NCIM-2931), S. aureus (NCIM-2079), K. pnuemoniae (NCIM-2719) and P. aeruginosa (NCIM-2053) bacterial strains using the Ditchplate and Well Diffusion Method. Among them, compound 6f was found to be active against all used bacterial strains. Objectives: Synthesis and study of antimicrobial activity of benzimidazole derivatives. Methods: Simple, known laboratory methods are used for the synthesis of all new benzimidazole derivatives (6a-f). Predicted bioactivity was studied using Molinspiration software. The antibacterial activity of synthesized derivatives was studied against E. coli (NCIM-2931), S. aureus (NCIM-2079), K. pnuemoniae (NCIM-2719) and P. aeruginosa (NCIM-2053) bacterial strains using Ditch-plate and Well diffusion methods. Results: We successfully synthesized new bis-benzimidazole derivatives using simple laboratory methods and studied their antimicrobial activity. Among the synthesized derivatives, N-((1H-benzimidazol-2-yl)methyl)-2-(pyridin-3-yl)-3H-benzimidazol-5-amine (6f) showed good activity against used bacterial strains. Conclusion: In this paper, we report the synthesis of novel and biological activity benzimidazole derivatives by a simple and efficient method. The carried out predicted bioactivity as well as actual bioactivity was reported, and it was observed that predicted bioactivity and actual antibacterial activity showed similar results. The incorporation of a pyridine ring in a benzimidazole derivative increased bioactivity.
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
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
黑糖珍珠完成签到 ,获得积分10
13秒前
Joanne完成签到 ,获得积分10
15秒前
sci_zt完成签到 ,获得积分10
22秒前
Spring完成签到,获得积分10
26秒前
航行天下完成签到 ,获得积分10
34秒前
祭酒完成签到 ,获得积分10
35秒前
美好灵寒完成签到 ,获得积分10
38秒前
蒲蒲完成签到 ,获得积分10
41秒前
zz完成签到 ,获得积分10
41秒前
潇潇完成签到,获得积分10
48秒前
roundtree完成签到 ,获得积分0
49秒前
kyokyoro完成签到,获得积分10
52秒前
52秒前
喵了个咪完成签到 ,获得积分10
57秒前
典雅三颜完成签到 ,获得积分10
58秒前
科研通AI2S应助shetianlang采纳,获得10
1分钟前
五月完成签到 ,获得积分10
1分钟前
uuuu完成签到 ,获得积分10
1分钟前
1分钟前
谭杰发布了新的文献求助10
1分钟前
shetianlang完成签到,获得积分10
1分钟前
小星星发布了新的文献求助10
1分钟前
1分钟前
xiuxiu_27完成签到 ,获得积分10
1分钟前
小高完成签到 ,获得积分10
2分钟前
zjzjzj123完成签到 ,获得积分10
2分钟前
su完成签到 ,获得积分10
2分钟前
猪仔5号完成签到 ,获得积分10
2分钟前
2分钟前
pluto应助独孤采纳,获得60
2分钟前
顺心的猪完成签到 ,获得积分10
2分钟前
2分钟前
yes完成签到 ,获得积分10
2分钟前
小星星完成签到,获得积分10
2分钟前
牟翎完成签到,获得积分10
2分钟前
橙子完成签到 ,获得积分10
2分钟前
小航完成签到 ,获得积分10
2分钟前
kanong完成签到,获得积分0
2分钟前
2分钟前
十一月的阴天完成签到 ,获得积分10
2分钟前
高分求助中
All the Birds of the World 4000
Production Logging: Theoretical and Interpretive Elements 3000
Animal Physiology 2000
Les Mantodea de Guyane Insecta, Polyneoptera 2000
Am Rande der Geschichte : mein Leben in China / Ruth Weiss 1500
CENTRAL BOOKS: A BRIEF HISTORY 1939 TO 1999 by Dave Cope 1000
Machine Learning Methods in Geoscience 1000
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 物理 生物化学 纳米技术 计算机科学 化学工程 内科学 复合材料 物理化学 电极 遗传学 量子力学 基因 冶金 催化作用
热门帖子
关注 科研通微信公众号,转发送积分 3736714
求助须知:如何正确求助?哪些是违规求助? 3280670
关于积分的说明 10020241
捐赠科研通 2997394
什么是DOI,文献DOI怎么找? 1644527
邀请新用户注册赠送积分活动 782060
科研通“疑难数据库(出版商)”最低求助积分说明 749656