Synthesis and bioactive evaluation of a novel series of coumarinazoles

被引：85

作者：

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

Cui, Sheng-Feng ^{[1
]}

Peng, Xin-Mei ^{[1
]}

Wen, Qin-Mei ^{[1
]}

Cai, Gui-Xin ^{[1
]}

Zhou, Cheng-He ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 15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：

Coumarin; Azole; Antibacterial; Antifungal; LogP; POTENTIAL ANTIMICROBIAL AGENTS; HUMAN SERUM-ALBUMIN; CALF THYMUS DNA; BIOLOGICAL EVALUATION; ALZHEIMERS-DISEASE; TRIAZOLES; DRUGS;

D O I：

10.1016/j.bmcl.2014.05.029

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 series of novel coumarinazoles were designed, synthesized, and characterized by IR, NMR, MS and HRMS spectra. The bioactive assay for the newly prepared compounds against six bacteria and five fungi manifested that most new compounds exhibited good or even stronger antibacterial and antifungal activities in comparison with reference drugs Chloromycin, Norfloxacin and Fluconazole. Bis-azole alcohols 7a and 7d-e showed better anti-Candida utilis activity than mono-azole derivatives 4a and 4d-e at the tested concentrations, and they were more potent than the clinical Fluconazole. While triazole alcohol 7a gave comparable anti-Candida albicans and anti-Candida mycoderma activity to Fluconazole and better anti-MRSA activity than mono-triazole one 4a and clinical Norfloxacin. 1H-Benzoimidazol-2-ylthio coumarin derivatives 4e and 7e gave the strongest anti-Escherichia coli JM109 efficacy. Oxiran-2-ylmethoxy moiety was found to be a beneficial fragment to improve antibacterial and antifungal activity to some extent. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：3605 / 3608

页数：4

共 20 条

[1]

A review on coumarins as acetylcholinesterase inhibitors for Alzheimer's disease [J].