The synthesis and activities of novel mononuclear or dinuclear cyclen complexes bearing azole pendants as antibacterial and antifungal agents

被引：36

作者：

Li, Shuo ^{[2
]}

Chen, Jia-Xuan ^{[1
]}

Xiang, Qing-Xiang ^{[1
]}

Zhang, Li-Qun ^{[1
]}

Zhou, Cheng-He ^{[3
]}

Xie, Jia-Qing ^{[2
]}

Yu, Lan ^{[2
]}

Li, Fang-Zhen ^{[2
]}

机构：

[1] Leshan Normal Univ, Dept Chem, Leshan 614000, Sichuan, Peoples R China

[2] Chongqing Univ Technol, Sch Chem Engn, Chongqing 400054, Peoples R China

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

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 84卷

基金：

美国国家科学基金会;

关键词：

Azoles; Cyclen; Antibacterial; Antifungal; Fluorescence spectrum; ANTIMICROBIAL ACTIVITY; CRYSTAL-STRUCTURE; SERUM-ALBUMIN; COPPER(II); BENZIMIDAZOLE; INHIBITORS; FLUORESCENCE; DERIVATIVES; MACROCYCLE; POLYMERS;

D O I：

10.1016/j.ejmech.2014.07.075

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel compounds containing 1,4,7,10-tetraazacyclododecane and azoles were synthesized and characterized by H-1 NMR, MS and elemental analysis. Bioactive assay manifested that some target compounds, such as 11a, 11b and 11d, displayed good and broad spectrum antimicrobial activities with relative low MIC values against most of tested strains. These dinuclear complexes gave comparable or even better antimicrobial efficiencies than the reference drugs Fluconazole and Chloromycin. The result showed that the metal ions were the key factors to enhance the antimicrobial activities for mononuclear or dinudear complexed in varying degrees. The interaction evaluation of compound lib with bovine serum albumin (BSA) as an example was tested by fluorescence method. The thermodynamic parameters indicated that the hydrogen bonds and van der waals forces played the major roles in the strong association between dinuclear compound and BSA. The CCK-8 tests also confirmed the safeties of these dinuclear compounds in vitro. (C) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：677 / 686

页数：10

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