Design, synthesis and biological evaluation of ciprofloxacin tethered bis-1,2,3-triazole conjugates as potent antibacterial agents

被引：75

作者：

Kant, Rama ^{[1
]}

Singh, Vishal ^{[1
]}

Nath, Gopai ^{[2
]}

Awasthi, Satish Kumar ^{[3
]}

Agarwal, Alka ^{[1
]}

机构：

[1] Banaras Hindu Univ, Inst Med Sci, Dept Med Chem, Varanasi 221005, Uttar Pradesh, India

[2] Banaras Hindu Univ, Inst Med Sci, Dept Microbiol, Varanasi 221005, Uttar Pradesh, India

[3] Univ Delhi, Dept Chem, Chem Biol Res Lab, Delhi 110007, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2016年 / 124卷

关键词：

1,2,3-Triazole conjugates; Ciprofloxacin; Antibacterial activity; Hemotoxicity; CLICK CHEMISTRY; 1,2,4-TRIAZOLE-CIPROFLOXACIN HYBRIDS; PIPERAZINYL QUINOLONES; MOLECULAR DOCKING; TRIAZOLE HYBRIDS; DERIVATIVES; ANALOGS; ANTIBIOTICS; 1,2,3-TRIAZOLES; RESISTANCE;

D O I：

10.1016/j.ejmech.2016.08.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of new bis-1,2,3-triazole linked ciprofloxacin conjugates was designed, synthesized and evaluated in vitro antibacterial activity against a panel of clinically relevant bacteria. A significant part of the compounds displayed enhanced activity against both Gram-positive and Gram-negative species of bacteria as compared to the parent drug. Additionally, negligible toxicity profile of compounds indicates that they may act a good antibiotic in future. Despite relatively small number of synthesized conjugates, it was possible to observe important dependences between their structure and activity. (C) 2016 Elsevier Masson SAS. All rights reserved.

引用

页码：218 / 228

页数：11

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