14049-94-6Relevant articles and documents
Evaluation of insulin‐like activity of novel zinc metal–organics toward adipogenesis signaling
Gabriel, Catherine,Tsave, Olga,Yavropoulou, Maria P.,Architektonidis, Theodore,Raptopoulou, Catherine P.,Psycharis, Vassilis,Salifoglou, Athanasios
, (2021)
Diabetes mellitus is a debilitating disease, plaguing a significant number of people around the globe. Attempts to develop new drugs on well‐defined atoxic metalloforms, which are capable of influencing fundamental cellular processes overcoming insulin resistance, has triggered an upsurge in molecular research linked to zinc metallodrugs. To that end, meticulous efforts were launched toward the design and synthesis of materials with insulin mimetic potential. Henceforth, trigonelline and N‐(2‐hydroxyethyl)‐iminodiacetic acid (HEIDAH2) were selected as organic substrates seeking binding to zinc (Zn(II)), with new crystalline compounds characterized by elemental analysis, FT‐IR, X‐rays, thermogravimetry (TGA), luminescence, NMR, and ESI‐MS spectrometry. Physicochemical characterization was followed by in vitro biochemical experiments, in which three out of the five zinc compounds emerged as atoxic, exhibiting bio‐activity profiles reflecting enhanced adipogenic potential. Concurrently, well‐defined qualitative–quantitative experiments provided links to genetic loci responsible for the observed effects, thereby unraveling their key involvement in signaling pathways in adipocyte tissue and insulin mimetic behavior. The collective results (a) signify the quintessential role of molecular studies in unearthing unknown facets of pathophysiological events in diabetes mellitus II, (b) reflect the close associations of properly configured molecular zincoforms to well‐defined biological profiles, and (c) set the stage for further physicochemical‐based development of efficient zinc antidiabetic metallodrugs.
Norfloxacin Zn(II)-based complexes: Acid base ionization constant determination, DNA and albumin binding properties and the biological effect against Trypanosoma cruzi
Gouvea, Ligiane R.,Martins, Darliane A.,Da Gama Jean Batista, Denise,De Nazaré C. Soeiro, Maria,Louro, Sonia R. W.,Barbeira, Paulo J. S.,Teixeira, Letícia R.
, p. 813 - 825 (2013)
Zn(II) complexes with norfloxacin (NOR) in the absence or in the presence of 1,10-phenanthroline (phen) were obtained and characterized. In both complexes, the ligand NOR was coordinated through a keto and a carboxyl oxygen. Tetrahedral and octahedral geometries were proposed for [ZnCl 2(NOR)]·H2O (1) and [ZnCl2(NOR)(phen)] ·2H2O (2), respectively. Since the biological activity of the chemicals depends on the pH value, pH titrations of the Zn(II) complexes were performed. UV spectroscopic studies of the interaction of the complexes with calf-thymus DNA (CT DNA) have suggested that they can bind to CT DNA with moderate affinity in an intercalative mode. The interactions between the Zn(II) complexes and bovine serum albumin (BSA) were investigated by steady-state and time-resolved fluorescence spectroscopy at pH 7.4. The experimental data showed static quenching of BSA fluorescence, indicating that both complexes bind to BSA. A modified Stern-Volmer plot for the quenching by complex 2 demonstrated preferential binding near one of the two tryptophan residues of BSA. The binding constants obtained (K b ) showed that BSA had a two orders of magnitude higher affinity for complex 2 than for 1. The results also showed that the affinity of both complexes for BSA was much higher than for DNA. This preferential interaction with protein sites could be important to their biological mechanisms of action. The analysis in vitro of the Zn(II) complexes and corresponding ligand were assayed against Trypanosoma cruzi, the causative agent of Chagas disease and the data showed that complex 2 was the most active against bloodstream trypomastigotes.
An effective non-chromatographic method for the purification of phenanthrolines and related ligands
Ferretti, Francesco,Ragaini, Fabio
, (2020)
1,10-Phenanthrolines are widely employed as ligands, but their use on a large scale is constrained by their difficult purification, which usually requires lengthy chromatographic separations. Herein, we describe a purification strategy that takes advantage of the high stability and low solubility of phenanthroline complexes to separate them from the by products of their synthesis. The formation of ZnCl2 complexes was employed, from which the free ligand can be recovered by reaction with aqueous NH3 in a biphasic CH2Cl2/H2O system. The same strategy was also successfully employed to purify related quinolino-guanidine ligands, demonstrating that the procedure is of general applicability.
Structures of 1: 1 Mononuclear Adducts of Zinc(ii) Halides, ZnX2 (X = Cl, Br, I) and of New Hydrates of 1: 1 Adducts of Zinc(ii) Nitrate and Sulfate with Aromatic N, N -Bidentate Base Derivatives of Pyridine (bpy, phen)
Bowmaker, Graham A.,Kim, Yang,Skelton, Brian W.,Sobolev, Alexandre N.,White, Allan H.
, p. 511 - 519 (2019/12/24)
Single crystal X-ray structure determinations have been executed for several title compounds of the mononuclear form [LMX2], namely [(bpy)ZnX2], X = Cl, Br; [(phen)ZnX2], X = Cl, Br, I (bpy = 2,2-bipyridine; phen = 1,10-phenanthroline). Also reported are
