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

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 α-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 Staphylococcus aureus, Bacillus subtilis and Xanthomonas campestris 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.

Mechanochemical synthesis and antiproliferative activity of novel ferrocene quinoline/quinolone hybrids

“…4,[12][13][14] The quinoline and quinolone N-heterocycles are privileged pharmacophores that play a pivotal role in the drug development process, having diverse biological properties, particularly antimalarial and anticancer activities. [15][16][17][18][19][20][21][22][23][24] A ferrocene-containing quinolone, ferroquine, was developed as an organometallic antimalarial F I G U R E 1 Rational behind the design of N-heterocycle ferrocene derivatives 5a-5d, 6a-6d, 7a, 7b, 8a, and 8b.…”

“…The quinoline and quinolone N ‐heterocycles are privileged pharmacophores that play a pivotal role in the drug development process, having diverse biological properties, particularly antimalarial and anticancer activities 15–24 . A ferrocene‐containing quinolone, ferroquine, was developed as an organometallic antimalarial agent currently undergoing Phase II human clinical trials 25 .…”