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氟喹诺酮类药物氟罗沙星的金属(II)配合物:合成、表征及生物学特性

Metal(II) Complexes of the Fluoroquinolone Fleroxacin: Synthesis, Characterization and Biological Profile.

作者信息

Kostelidou Alexandra, Perdih Franc, Kljun Jakob, Dimou Foteini, Kalogiannis Stavros, Turel Iztok, Psomas George

机构信息

Department of General and Inorganic Chemistry, Faculty of Chemistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Greece.

Faculty of Chemistry and Chemical Technology, University of Ljubljana, Večna pot 113, 1000 Ljubljana, Slovenia.

出版信息

Pharmaceutics. 2022 Apr 20;14(5):898. doi: 10.3390/pharmaceutics14050898.

DOI:10.3390/pharmaceutics14050898
PMID:35631484
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9144902/
Abstract

A series of complexes of divalent transition metals (Cu(II), Mn(II), Zn(II), Co(II) and Ni(II)) with the quinolone antibacterial agent fleroxacin, in the absence or presence of an -diimine such as 2,2'-bipyridine, 1,10-phenanthroline or 2,2'-bipyridylamine, were prepared and characterized. The complexes were characterized by various physicochemical and spectroscopic techniques and by single-crystal X-ray crystallography. The in vitro antibacterial activity of the complexes was studied against the bacterial strains , and and was higher than that of free quinolone. The affinity of the complexes for bovine and human serum albumin was studied by fluorescence emission spectroscopy and the determined binding constants showed tight and reversible binding to the albumins. The interaction of the complexes with calf-thymus DNA was studied by various techniques, which showed that intercalation was the most plausible mode of interaction.

摘要

制备并表征了一系列二价过渡金属(铜(II)、锰(II)、锌(II)、钴(II)和镍(II))与喹诺酮类抗菌剂氟罗沙星形成的配合物,这些配合物是在不存在或存在如2,2'-联吡啶、1,10-菲啰啉或2,2'-联吡啶胺等二亚胺的情况下形成的。通过各种物理化学和光谱技术以及单晶X射线晶体学对这些配合物进行了表征。研究了这些配合物对细菌菌株、和的体外抗菌活性,其活性高于游离喹诺酮。通过荧光发射光谱研究了配合物与牛血清白蛋白和人血清白蛋白的亲和力,测定的结合常数表明它们与白蛋白紧密且可逆地结合。通过各种技术研究了配合物与小牛胸腺DNA的相互作用,结果表明嵌入是最可能的相互作用模式。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/7806eabff778/pharmaceutics-14-00898-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/d6f80a16c331/pharmaceutics-14-00898-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/723cee114d22/pharmaceutics-14-00898-sch001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/2e74cf93584f/pharmaceutics-14-00898-g003a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/258981557a5d/pharmaceutics-14-00898-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/5e74d255cdcf/pharmaceutics-14-00898-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/193d8220473f/pharmaceutics-14-00898-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/192d73b1b144/pharmaceutics-14-00898-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/7806eabff778/pharmaceutics-14-00898-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/d6f80a16c331/pharmaceutics-14-00898-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/723cee114d22/pharmaceutics-14-00898-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/55aca82059e3/pharmaceutics-14-00898-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/2e74cf93584f/pharmaceutics-14-00898-g003a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/258981557a5d/pharmaceutics-14-00898-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/5e74d255cdcf/pharmaceutics-14-00898-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/193d8220473f/pharmaceutics-14-00898-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/192d73b1b144/pharmaceutics-14-00898-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af5d/9144902/7806eabff778/pharmaceutics-14-00898-g008.jpg

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A New Calcium(II)-Based Substitute for Enrofloxacin with Improved Medicinal Potential.一种具有更高药用潜力的新型基于钙(II)的恩诺沙星替代物。
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