Synthesis and antibacterial activity of N-[2-[5-(methylthio)thiophen-2-yl]-2-oxoethyl] and N-[2-[5-(methylthio)thiophen-2-yl]-2-(oxyimino)ethyl]piperazinylquinolone derivatives

被引：38

作者：

Foroumadi, A

Oboudiat, M

Emami, S

Karimollah, A

Saghaee, L

Moshafi, MH

Shafiee, A ^{[1
]}

机构：

[1] Univ Tehran Med Sci, Fac Pharm, Tehran 14174, Iran

[2] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran 14174, Iran

[3] Isfahan Univ Med Sci, Fac Pharm, Dept Med Chem, Esfahan, Iran

[4] Mazandaran Univ Med Sci, Fac Pharm, Dept Med Chem, Sari, Iran

[5] Kerman Univ Med Sci, Fac Pharm, Kerman, Iran

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 10期

关键词：

quinolones; N-substituted piperazinylquinolones; in vitro antibacterial activity;

D O I：

10.1016/j.bmc.2005.12.058

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

A number of N-substituted piperazinylquinolone derivatives were synthesized and evaluated for antibacterial activity against Gram-positive and Gram-negative bacteria. Preliminary results indicated that most compounds tested in this study demonstrated comparable or better activity against Staphylococcus aureus and Staphylococcus epidermidis than their parent piperazinylquinolones as reference drugs. Among these derivatives, ciprofloxacin derivative 5a, containing N-[2-[5-(methylthio)thiophen-2-yl]-2-oxoethyl] residue, showed significant improvement of potency against staphylococci, maintaining Gram-negative coverage. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：3421 / 3427

页数：7

共 35 条

[1]

The future of the quinolones [J].