[en] Chromene and spirocyclic 2-oxindole derivatives were readily synthesized in good yields via a one-pot three-component reaction involving Knoevenagel condensation of aromatic aldehyde or isatin with an active methylene reagent then the intermediate was reacted with another different active methylene reagent via a DABCO-catalysed Michael addition to yield the main products. Some advantages of this protocol are good yields, use of available catalysts, simple workup procedure and short reaction times. All synthesized products were characterized by FT-IR, 1H- and 13C-NMR spectroscopy. (author)

[en] Natural polymers, extracted from plants, can be used as coagulants for water treatment in addition to metal salts and synthetic polymers. Natural materials may offer benefits such as local production, lesser health hazards and affordability for developing world. Opuntia stricta plant, a cactus specie native to Mexico, has been explored in this study for its efficacy as coagulant. Efficiency of Opuntia stricta was assessed on the basis of turbidity removal from lab prepared and surface water samples. The effect of water pH on its performance was also analyzed. The study results revealed that removal efficiency of Opuntia stricta for turbidity removal remains consistent within a wide pH range (pH 5 to 10), in contrast to other coagulants which are pH dependent. Furthermore, pH of the water remains constant during coagulation and pH adjustment may not be required for subsequent treatment processes, which is often needed in case metal coagulants are used. Residual turbidity below 20 NTU is conveniently achieved by using Opuntia stricta even when it is used at very low doses. Formation of exceptionally large flocs and their linear configuration reveals the possibility that mechanism of coagulation by Opuntia stricta is adsorption and inter-particle bridging. (author)

[en] Pharmacological testing of 1,3,4-thiadiazine, which are synthesized on the basis of derivatives of acetylenic alcohols on white rats in vivo, showed that they have anticoagulant properties in relation to human blood. (author)

[en] The synthesis of deuterium labelled 4'-,6-,7- and 8-hydroxy metabolites of warfarin and phenprocoumon is described. The pentadeuterio labelled 6-,7- and 8-hydroxyphenprocoumons were prepared via alkylation of the respective 6-, 7- and 8-methoxy-4-hydroxycoumarins with 1-(phenyl-d₅)-1-bromopropane and subsequent cleavage of the methyl protecting group with boron tribromide. The synthesis of 1-(pentadeuteriophenyl)-1-bromopropane and the 6-, 7- and 8-methoxy-4-hydroxycoumarins are also presented. The pentadeuterio labelled 6-, 7- and 8-hydroxywarfarins were obtained by reaction of 4-(phenyl-d₅)-3-buten-2-one with the respective 6-, 7- and 8-hydroxy-4-hydroxycoumarins in methanol followed by hydrolysis of the intermediate cyclic methyl ketals in aqueous acid. 4-Hydroxycoumarin-5,6,7,8-d₄, prepared from phenyl-d₆ and tetradeuteriomalonic acid, was reacted with 1-(p-hydroxyphenyl)-1-propanol and 4-(p-hydroxyphenyl)-3-buten-2-one to yield labelled 4'-hydroxyphenprocoumon and 4'-hydroxywarfarin respectively. (author)

[en] The following experiments were planned to look at the effects of water-droplets sizes and radiation field on the migration of volatile I₂ and CH₃I that may occur during an accident in the nuclear-reactor containment. 0, 38, 42, and 48 μm sizes of water droplets could be generated when 0, 80, 60, and 40 kHz frequencies were applied at a nominal operating condition (20 μm orifice diameter, 20 cm³ syringe capacity, 8.2 x 10-4 cm/s syringe pump run speed, and 0.139 cm³/min liquid feed rate). The formed monodisperse water droplets were well dispersed with 15 x 100 cm³/min air and diluted 40 L/min air before significant coagulation occurs. Gases of I₂ and CH₃I were generated at about 60.deg.C and room temperature respectively and then led to the cylindrical water jet with the volumetric flowrate of 5cc/min. The amount of transferred gaseous iodine by adsorption on water droplets was strongly influenced by the existence of water. CH₃I and H₂O can decompose into various chemical species on exposure to external radiation, so a transferred amount of CH₃I on water droplets were lower under the combination of 10 μCi Na-22, 1 μCi Cd-109, 1 μCi Cs-137, and 1 μCi Co-57 radioactive source discs than the case of absence of the radiation condition as shown in Figure 2. However, a relationship between the transferred volatile CH₃I concentrations and water droplet sizes showed the same trend to the case of absence of the radiation condition. Hydrolysis reaction rates of I₂ and CH₃I with water are very slow in comparison with physical weathering and physical dissolution, and they are only slightly soluble in water.

[en] Response surface method and experimental design were applied as alternatives to the conventional methods for optimization of the coagulation test. A central composite design was used to build models for predicting and optimizing the coagulation process. The model equations were derived using the least square method of the Minitab 16 software. In these equations, the removal efficiency of turbidity and COD were expressed as second-order functions of the coagulant dosage and coagulation pH. By applying RSM, the optimum condition using PFPD_1 was coagulant dosage of 384 mg/L and coagulation pH of 7.75. The optimum condition using PFPD_2 was coagulant dosage of 390 mg/L and coagulation pH of 7.48. Confirmation experiment demonstrated a good agreement between experimental values and model predicted. This demonstrates that RSM and CCD can be successfully applied for modeling and optimizing the coagulation process using PFPD_1 and PFPD_2

[en] Highlights: • Rodenticide exposure increased with the contribution of urban habitat. • Red kites and urban goshawks were at greatest risk for rodenticide poisoning. • Rodenticide exposure may not be limited to terrestrial food webs. • Ibuprofen and fluoroquinolones were the most frequently detected medicinal products. • Most analysed and currently used plant protection products were not detected. Intensification of agricultural practices has resulted in a substantial decline of Europe's farmland bird populations. Together with increasing urbanisation, chemical pollution arising from these land uses is a recognised threat to wildlife. Raptors are known to be particularly sensitive to pollutants that biomagnify and are thus frequently used sentinels for pollution in food webs. The current study focussed on anticoagulant rodenticides (ARs) but also considered selected medicinal products (MPs) and frequently used plant protection products (PPPs). We analysed livers of raptor species from agricultural and urban habitats in Germany, namely red kites (MIML; Milvus milvus), northern goshawks (ACGE; Accipiter gentilis) and Eurasian sparrowhawks (ACNI; Accipiter nisus) as well as white-tailed sea eagles (HAAL; Haliaeetus albicilla) and ospreys (PAHA; Pandion haliaetus) to account for potential aquatic exposures. Landscape composition was quantified using geographic information systems. The highest detection of ARs occurred in ACGE (81.3%; n = 48), closely followed by MIML (80.5%; n = 41), HAAL (38.3%; n = 60) and ACNI (13%; n = 23), whereas no ARs were found in PAHA (n = 13). Generalized linear models demonstrated (1) an increased probability for adults to be exposed to ARs with increasing urbanisation, and (2) that species-specific traits were responsible for the extent of exposure. For MPs, we found ibuprofen in 14.9% and fluoroquinolones in 2.3% in individuals that were found dead. Among 30 investigated PPPs, dimethoate (and its metabolite omethoate) and thiacloprid were detected in two MIML each. We assumed that the levels of dimethoate were a consequence of deliberate poisoning. AR and insecticide poisoning were considered to represent a threat to red kites and may ultimately contribute to reported decreased survival rates. Overall, our study suggests that urban raptors are at greatest risk for AR exposure and that exposures may not be limited to terrestrial food webs.

[en] In an MRI study examining anomalies of the septum pellucidum in 505 cases, we detected bilateral septum formation of the lateral ventricles in a 17-months-old-baby. In this study, we evaluate 505 (242 males and 263 females) patients referred to the Emaray Imaging Center, Ankara, Turkey with various prediagnoses. We specially selected all the cases from a non-psychotic population. We obtained MRI scans on a 1-Tesla imager (Picker International, Highland Heights, Ohio, USA), with slices of 5 and 6 mm thickness. In the axial and coronal sections, we observed septum formation laterally between the anterior horn and the ventricular body of the lateral ventricles. Radio opaque septum formations started from the caudate nucleus and stretched to the genu of the corpus callosum. There was a second septum formation between the posterior horn and the ventricular body of the right lateral ventricle. It started from the caudate nucleus and stretched to the cavum vergae. (author)

[en] Objective: To investigate the Bioequivalence of Anplag® 90mg (Ticagrelor) tablet and Brilinta® 90 mg (Ticagrelor) tablet under fasting conditions in healthy Pakistani subjects. Method: This was an open-label, cross-over, randomized, single-dose, two-period, single-center Bioequivalence Study conducted at Center of Bioequivalence Studies and Clinical Research (CBSCR), ICCBS, University of Karachi, Karachi, Pakistan from September 2020 to January 2021. This was an open-label, randomized, single-dose, two-period, crossover Bioequivalence Study. After randomization, a single dose of Ticagrelor 90mg tablet (test or reference drug) were administered orally in 1:1 ratio to each subject under fasting conditions. Seven days washout period was kept between the two periods in order to avoid carry over. Blood samples were then taken up to 48th hours postdose. Point estimates and 90% confidence intervals (CI) for the ratio of the log-transformed values were calculated. Bioequivalence assessment of both, the reference and the test drugs were based on the primary Pharmacokinetic PK metrics including peak maximum concentration (Cmax), area under the curve (AUC) from zero to last quantifiable concentration (AUClast), and AUC from zero to infinity (AUCtotal) after log-transformation of data with ANOVA. In this bioequivalence study, the primary pharmacokinetic parameters were assessed for both Ticagrelor and its Active Metabolite (AR-C124910XX). Safety endpoints were evaluated by monitoring adverse events (AEs). Results: The 90% Confidence Intervals (CIs) of the Geometric Mean Ratio for primary PK parameters including Cmax, AUClast, and AUCtotal all were within the accepted bioequivalence range of 80%- 125%. In the current study, no serious adverse events were reported. Conclusion: Our results showed that the two tested formulations of Ticagrelor tablets were bioequivalent and well tolerated. (author)

[en] The ideal oral anticoagulant agent during catheter ablation (CA) for atrial fibrillation (AF) remained unclear.