Synthesis and biological evaluation of a class of quinolone triazoles as potential antimicrobial agents and their interactions with calf thymus DNA

被引：120

作者：

Cui, Sheng-Feng ^{[1
]}

Ren, Yu ^{[1
]}

Zhang, Shao-Lin ^{[1
]}

Peng, Xin-Mei ^{[1
]}

Damu, Guri L. V. ^{[1
]}

Geng, Rong-Xia ^{[1
]}

Zhou, Cheng-He ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 11期

基金：

高等学校博士学科点专项科研基金; 中国国家自然科学基金;

关键词：

Quinolone; Triazole; Antibacterial; Antifungal; DNA; ANTIBACTERIAL ACTIVITY; STRUCTURAL INSIGHT; SERUM-ALBUMIN; DERIVATIVES; BINDING; COMPLEX; DESIGN; DRUGS;

D O I：

10.1016/j.bmcl.2013.03.118

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

A novel series of quinolone triazoles were synthesized and characterized by IR, NMR, MS and HRMS spectra. All the newly prepared compounds were screened for their antimicrobial activities against seven bacteria and four fungi. Bioactive assay manifested that most of new compounds exhibited good or even stronger antibacterial and antifungal activities against the tested strains including multi-drug resistant MRSA in comparison with reference drugs Norfloxacin, Chloromycin and Fluconazole. The preliminary interactive investigations of compound 6b with calf thymus DNA by fluorescence and UV-vis spectroscopic methods revealed that compound 6b could effectively intercalate DNA to form compound 6b-DNA complex which might block DNA replication and thus exert its antimicrobial activities. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：3267 / 3272

页数：6

共 25 条

[1]

Fluorescence Interaction and Determination of Calf Thymus DNA with Two Ethidium Derivatives [J].