1,2,3-Triazole-derived naphthalimides as a novel type of potential antimicrobial agents: Synthesis, antimicrobial activity, interaction with calf thymus DNA and human serum albumin

被引：79

作者：

Lv, Jing-Song ^{[1
,2
]}

Peng, Xin-Mei ^{[1
]}

Kishore, Baathulaa ^{[1
]}

Zhou, Cheng-He ^{[1
]}

机构：

[1] Southwest Univ, Sch Chem & Chem Engn, Lab Bioorgan & Med Chem, Chongqing 400715, Peoples R China

[2] Bijie Univ, Sch Chem & Chem Engn, Guizhou 551700, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 01期

基金：

中国国家自然科学基金; 高等学校博士学科点专项科研基金;

关键词：

Antibacterial; Triazole; Human serum albumin; Naphthalimide; DNA; BIOLOGICAL EVALUATION; ANTIBACTERIAL; DERIVATIVES; ANTIFUNGAL; AZOLES; TRIAZOLES; DYNAMICS; ANALOGS; COMPLEX; DESIGN;

D O I：

10.1016/j.bmcl.2013.11.013

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1,2,3-triazole-derived naphthalimides as a novel type of potential antimicrobial agents were synthesized and characterized by IR, NMR and HRMS spectra. All the new compounds were screened for their antimicrobial activity against four Gram-positive bacteria, four Gram-negative bacteria and three fungi. Bioactive assay manifested that 3,4-dichlorobenzyl compound 9e and its corresponding hydrochloride 11e showed better anti-Escherichia coli activity than Norfloxacin and Chloromycin. Preliminary research revealed that compound 9e could effectively intercalate into calf thymus DNA to form compound 9e-DNA complex which might block DNA replication and thus exert antimicrobial activities. Human serum albumin could effectively store and carry compound 9e by electrostatic interaction. (C) 2013 Published by Elsevier Ltd.

引用

页码：308 / 313

页数：6

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