Efthimiadou Eleni K, Psomas George, Sanakis Yiannis, Katsaros Nikos, Karaliota Alexandra
Institute of Physical Chemistry, NCSR "Demokritos", GR-15310 Aghia Paraskevi Attikis, Greece.
J Inorg Biochem. 2007 Mar;101(3):525-35. doi: 10.1016/j.jinorgbio.2006.11.020. Epub 2006 Dec 3.
Nine new metal complexes of the quinolone antibacterial agent N-propyl-norfloxacin, pr-norfloxacin, with VO(2+), Mn(2+), Fe(3+), Co(2+), Ni(2+), Zn(2+), MoO(2)(2+), Cd(2+) and UO(2)(2+) have been prepared and characterized with physicochemical and spectroscopic techniques while molecular mechanics calculations for Fe(3+), VO(2+) and MoO(2)(2+) 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)(H(2)O) 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 UO(2)(pr-norf)(2) which shows better inhibition against S. aureus.
已制备了喹诺酮类抗菌剂 N-丙基-诺氟沙星（pr-诺氟沙星）与 VO(2+)、Mn(2+)、Fe(3+)、Co(2+)、Ni(2+)、Zn(2+)、MoO(2)(2+)、Cd(2+)和 UO(2)(2+)形成的九种新型金属配合物，并采用物理化学和光谱技术对其进行了表征，同时对 Fe(3+)、VO(2+)和 MoO(2)(2+)配合物进行了分子力学计算。在所有配合物中，pr-诺氟沙星作为双齿去质子化配体，通过吡啶酮和一个羧酸根氧原子与金属结合。所有配合物均为六配位，八面体几何结构略有畸变。对于配合物 VO(N-丙基-诺氟沙星基)(2)(H(2)O)，与钒氧基相对的轴向位置被一个吡啶酮氧原子占据。已采用多种光谱技术研究了这些配合物与小牛胸腺 DNA 的相互作用，结果表明这些配合物可与小牛胸腺 DNA 结合，导致 B 型向 A 型 DNA 转变。已对这些配合物对三种不同微生物的抗菌活性进行了测试。除 UO(2)(pr-norf)(2)对金黄色葡萄球菌表现出更好的抑制作用外，这些配合物与游离的 pr-诺氟沙星相比，生物活性相同或降低。
