Metal complexes with the quinolone antibacterial agent N-propyl-norfloxacin: Synthesis, structure and bioactivity

详细信息	查看全文 | 推荐本文 |

• 作者：Eleni K. Efthimiadou ; George Psomas ; Yiannis Sanakis ; Nikos Katsaros ; Alex ; ra Karaliota
• 关键词：N-propyl-norfloxacin ; Quinolones ; Metal complexes ; Molecular modeling ; Interaction with calf-thymus DNA ; MIC
• 刊名：Journal of Inorganic Biochemistry
• 出版年：2007
• 期刊代码：53_01620134
• 类别：ch
• 出版时间：March 2007
• 卷：101
• 期：3
• 页码：525-535
• 文件大小：358 K

摘要

Nine new metal complexes of the quinolone antibacterial agent N-propyl-norfloxacin, pr-norfloxacin, with VO²⁺, Mn²⁺, Fe³⁺, Co²⁺, Ni²⁺, Zn²⁺, , Cd²⁺ and have been prepared and characterized with physicochemical and spectroscopic techniques while molecular mechanics calculations for Fe³⁺, VO²⁺ and complexes have been performed. In all complexes, pr-norfloxacin acts as a bidentate deprotonated ligand bound to the metal through the pyridone and one carboxylate oxygen atoms. All complexes are six-coordinate with slightly distorted octahedral geometry. For the complex VO(N-propyl-norfloxacinato)₂(H₂O) the axial position, trans to the vanadyl oxygen, is occupied by one pyridone oxygen atom. The investigation of the interaction of the complexes with calf-thymus DNA has been performed with diverse spectroscopic techniques and has shown that the complexes can be bound to calf-thymus DNA resulting to a B → A DNA transition. The antimicrobial activity of the complexes has been tested on three different microorganisms. The complexes show equal or decreased biological activity in comparison to the free pr-norfloxacin except UO₂(pr-norf)₂ which shows better inhibition against S. aureus.