Antioxidant status in the vitreous of eyes with rhegmatogenous retinal detachment with and without proliferative vitreoretinopathy, macular hole and epiretinal membrane

(1) Background: The aim of the study was to test the hypothesis that the antioxidant status in the vitreous body of eyes, which had been vitrectomized due to rhegmatogenous retinal detachment (RRD) with or without proliferative vitreoretinopathy (PVR), is higher than in eyes vitrectomized due to other retinal diseases. (2) Methods: four patient groups were analyzed: 22 eyes of patients with RRD without PVR, 27 eyes with RRD and PVR, 22 eyes with macular hole (MH) and 10 eyes with epiretinal membrane (ERM). Spectrophotometric methods were used to determine the total antioxidant status (TAS) values as well as superoxide dismutase (SOD) and glutathione reductase (GR) activities in the vitreous fluid samples. (3) Results: no significant differences in TAS values and antioxidant enzyme activities were observed among patient with RRD with and without PVR and with MH and ERM. The longer the duration of RRD leading to PVR and better postoperative visual acuity, the higher the TAS level. No significant differences were found between “macula on” and “macula off” subgroups within the RRD group and the RRD combined with PVR group. (4) Conclusions: The preliminary results do not support the thesis that the antioxidant status of vitrectomized eyes is different in patients with RRD with or without PVR in comparison to patients with MH and ERM. In patients with RRD, PVR presence and detached macula do not affect the values of TAS, SOD and GR in the vitreous fluid. The duration of the disease influences TAS in the vitreous in eyes with RRD complicated with PVR

4-({(E)-[2-(But-3-en-1-yl)-1-(prop-2-en-1-yl)-4-sulfanyl-1H-imidazol-5-yl]methyl­idene}amino)-3-phenyl-1H-1,2,4-triazole-5(4H)-thione

In the title compound, C19H20N6S2, the dihedral angle between the phenyl and triazole rings is 24.1 (2)° while the dihedral angles between the imidazole ring and the triazole and phenyl rings are 39.9 (2) and 55.3 (2)°, respectively. The crystal structure is stabilized by inter­molecular N—H⋯N hydrogen bonds which form chains along [10]

Antioxidants in the retina and vitreous — current state of knowledge

In the healthy organism, there is a constant balance between the formation and neutralization of free radicals. Oxidative stress is a result of free radicals’ production and naturalization imbalance, in favor of the free radicals’ high concentration. Literature suggests the existence of the relationship between decreased intraocular antioxidant capacity and ocular diseases. Retina and the photoreceptors in particularl, are susceptible to oxygen deficiency due to their great oxygen consumption. The aim of this review was to describe the relationship between oxidative stress and the most common vitreoretinal disorders. The authors focused on four ocular diseases such as vitreous degeneration, rhegmatogenous retinal detachment, age-related macular degeneration and diabetic retinopathy. It was widely proven that high oxidative stress damages retina by the acceleration of photoreceptors and ganglion cells apoptosis. Available data suggesting that substances scavenging oxidative stress may be effective in slowing down the progression of these degenerative ocular diseases. However, the effects of antioxidants treatment are ambiguous, successful results of experimental studies lead straight to clinical use in human in the future

4-Amino-3-(1-naphthyl­oxymeth­yl)-1H-1,2,4-triazole-5(4H)-thione

In the title compound, C13H12N4OS, the dihedral angle between the triazole and naphthalene ring systems is 67.42 (5)°. In the crystal, adjacent mol­ecules are linked via two pairs of inter­molecular N—H⋯S inter­actions, forming R 2 2(8) and R 2 2(10) ring motifs. Weak C—H⋯S inter­actions generate infinite chains along [001] and the structure is further consolidated by C–H⋯π bonds and aromatic π⋯π stacking inter­actions [distance between the centroids of the triazole rings = 3.2479 (7) Å]

Synthesis, characterization and antibacterial activity studies of new 2‑pyrral‑L‑amino acid Schif base palladium (II) complexes.

Three new 2-pyrral amino acid Schif base palladium (II) complexes were synthesized, characterized and their activity against six bacterial species was investigated. The ligands: Potassium 2-pyrrolidine-L-methioninate (L1), Potassium 2-pyrrolidine-L-histidinate (L2) and Potassium 2-pyrrolidine-L-tryptophanate (L3) were synthesized and reacted with dichloro(1,5- cyclooctadiene)palladium(II) to form new palladium (II) complexes C1, C2 and C3, respectively. 1 NMR, FTIR, UV–Vis,elemental analysis and conductivity measurements were used to characterize the products. The antibacterial activities of the compounds were evaluated against Gram-positive Staphylococcus aureus (S. aureus, ATCC 25923), methicillin-resistant Staphylococcus aureus (MRSA, ATCC 33591), Staphylococcus epidermidis (S. epidermidis, ATCC 12228) and Streptococcus pyogenes (S. pyogenes, ATCC 19615) and, gram-negative Pseudomonas aeruginosa (P. aeruginosa, ATCC 27853) and Klebsiella pneumoniae (K. pneumoniae, ATCC 13883) using the agar well difusion assay and microtitre plate serial dilution method. The palladium complexes were active against the selected bacteria with the imidazole ring containing complex C2 and indole heterocyclic ring containing complex C3 showing the highest activity

An Insight into Fluorinated Imines and Hydrazones as Antibacterial Agents

Fluorinated imines (Schiff bases) and fluorinated hydrazones are of particular interest in medicinal chemistry due to their potential usefulness in treating opportunistic strains of bacteria that are resistant to commonly used antibacterial agents. The present review paper is focused on these fluorinated molecules revealing strong, moderate or weak in vitro antibacterial activities, which have been reported in the scientific papers during the last fifteen years. Fluorinated building blocks and reaction conditions used for the synthesis of imines and hydrazones are mentioned. The structural modifications, which have an influence on the antibacterial activity in all the reported classes of fluorinated small molecules, are highlighted, focusing mainly on the importance of specific substitutions. Advanced research techniques and innovations for the synthesis, design and development of fluorinated imines and hydrazones are also summarized

TG-DSC and TG-FTIR Studies of Annelated Triazinylacetic Acid Ethyl Esters—Potential Anticancer Agents

To avoid problems associated with the storage and processing of newly developed potential medicines, there is a need to carry out thermal studies in the preclinical phase of drug development. The thermal behaviour and decomposition pathway of a whole novel class of patented potential molecular pharmaceutics, i.e., ethyl 2-[4-oxo-8-(R-phenyl)-4,6,7,8-tetrahydroimidazo[2,1-c][1,2,4]triazin-3-yl]acetates (1–6) were reported for the first time in inert and oxidative atmospheres. The experiments were conducted with the use of simultaneous thermogravimetry/differential scanning calorimetry (TG-DSC) and simultaneous thermogravimetry coupled with Fourier transform infrared spectroscopy (TG-FTIR). The decomposition pathways of compounds 1–6 were found to be different under oxidative and inert conditions. It was proven that the investigated molecules reveal higher thermal stability under a synthetic air atmosphere than under a nitrogen atmosphere, and their decomposition is preceded by the melting process. Among all the investigated compounds, only the meta-chloro derivative (4) was found to exhibit interesting polymorphic behaviour at a low heating rate (10 °C min−1). It was proven that the oxidative decomposition process of the studied molecules proceeds in three overlapping stages accompanied by strong exothermic effects. Additionally, it was concluded that the title compounds were stable up to a temperature of 195–216 °C in an atmosphere of synthetic air, and their thermal stability decreased in the order of R at the benzene ring: 4-CH3 > 3,4-Cl2 > 4-Cl > H > 2-OCH3 > 3-Cl

Combined Micellar Liquid Chromatography Technique and QSARs Modeling in Predicting the Blood–Brain Barrier Permeation of Heterocyclic Drug-like Compounds

The quantitative structure–activity relationship (QSAR) methodology was used to predict the blood–brain permeability (log BB) for 65 synthetic heterocyclic compounds tested as promising drug candidates. The compounds were characterized by different descriptors: lipophilicity, parachor, polarizability, molecular weight, number of hydrogen bond acceptors, number of rotatable bonds, and polar surface area. Lipophilic properties of the compounds were evaluated experimentally by micellar liquid chromatography (MLC). In the experiments, sodium dodecyl sulfate (SDS) as the effluent component and the ODS-2 column were used. Using multiple linear regression and leave-one-out cross-validation, we derived the statistically significant and highly predictive quantitative structure–activity relationship models. Thus, this study provides valuable information on the expected properties of the substances that can be used as a support tool in the design of new therapeutic agents

Pékin - Paris : l'étudiant chinois est-il une marchandise ?

Au moment où le gouvernement français tente d'enrayer l'immigration clandestine chinoise en choisissant la coopération avec Pékin, des milliers d'étudiants chinois cherchent chaque année à rejoindre cette France "romantique" dont on leur a tant parlé.Sztanke Michaël. Pékin - Paris : l'étudiant chinois est-il une marchandise ?. In: Hommes et Migrations, n°1254, Mars-avril 2005. Chinois de France. pp. 74-81