A new efficient route to 7-aryl-6-fluoro-8-nitroquinolones as potent antibacterial agents

被引：12

作者：

Al-Trawneh, Salah A. ^{[1
]}

El-Abadelah, Mustafa M. ^{[2
]}

Al-Abadleh, Mohammad M. ^{[3
]}

Zani, Franca ^{[4
]}

Incerti, Matteo ^{[4
]}

Vicini, Paola ^{[4
]}

机构：

[1] Mutah Univ, Dept Chem, Fac Sci, Al Karak 61710, Jordan

[2] Univ Jordan, Dept Chem, Fac Sci, Amman 11942, Jordan

[3] Taibah Univ, Coll Pharm, Al Madinah 41477, Saudi Arabia

[4] Univ Parma, Dipartimento Farm, I-43124 Parma, Italy

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 86卷

关键词：

7-Aryl-6-fluoro-8-nitroquinolones; 7-Aryl-1-cyclopropyl-6-fluoro-8-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylic acids; Suzuki-Miyaura reaction; Antibacterial activity; CROSS-COUPLING REACTIONS;

D O I：

10.1016/j.ejmech.2014.08.065

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 7-aryl-6-fluoro-8-nitroquinolones (6a-e) were synthesized through a novel, simple and clean synthetic procedure, through a Suzuki-Miyaura reaction. The target compounds were evaluated in vitro for their antimicrobial properties against bacterial and fungal strains. All of them showed antibacterial activity higher than the activity of ciprofloxacin, both towards Gram positive Bacillus subtilis and Staphylococcus aureus, and Gram negative Haemophilus influenzae strains. Compound 6d, containing the trisubstituted 7-aryl moiety, emerged as the most active quinolone derivative with MIC values ranging from 0.00007 mu g/mL to 0.015 mu g/mL. (C) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：364 / 367

页数：4

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