Synthesis and antibacterial activity of novel levofloxacin derivatives containing a substituted thienylethyl moiety

• Published in: Daru 2012-08, Vol.20 (8), p.1-1
• Main Authors: Mohammadhosseini, Negar, Alipanahi, Zahra, Alipour, Eskandar, Emami, Saeed, Faramarzi, Mohammad Ali, Samadi, Nasrin, Khoshnevis, Nika, Shafiee, Abbass, oumadi, Alireza
• Format: Article
• Language: English
• Subjects: Acids; Bacteria; Gram-negative bacteria; Gram-positive bacteria; Infections
• ISSN: 1560-8115; 2008-2231

Piperazinyl quinolones such as ciprofloxacin, ofloxacin and levofloxacin are an important group of quinolone antimicrobials which are widely used in the treatment of various infectious diseases. In the present study, the authors synthesized a new series of levofloxacin derivatives and evaluated their antibacterial activities. The N-substituted analogs of levofloxacin 6a-j were prepared by nucleophilic reaction of N-desmethyl levofloxacin 11 with thienylethyl bromide derivatives 8 or 9. All target compounds were tested using conventional agar dilution method in comparison to levofloxacin and N-desmethyl levofloxacin and their MIC values were determined against a panel of Gram-positive and Gram-negative bacteria. The authors have designed and synthesized novel quinolone derivatives bearing functionalized thienylethyl moiety on the piperazine ring of levofloxacin. The results of antibacterial screening against Gram-positive and Gram-negative bacteria revealed that the introduction of functionalized thienylethyl moiety on the piperazine ring of levofloxacin can improve the activity against Gram-positive bacteria. Gram-positive bacteria are responsible for a wide range of infectious diseases, and rising resistance in this group is causing increasing concern.