Sulfanyl chloride induced heterocyclization of N-(pyrazolyl)styrylacetamides

Heterocyclization of N-(pyrazol-3-yl)styrylacetamides with arenesulfenyl chlorides yields the corresponding tetrahydrofuran-2-iminium perchlorates isolable after chromatography as trans-5-aryl-4-(arylthio)tetrahydrofuran-2-ones and 5-aryl-4-(arylthio)-1-(pyrazol-3-yl)pyrrolidin-2-ones, with the latter predominating. N-(Pyrazol-4-yl)styrylacetamides react under analogous conditions to give 5-aryl-4-(arylthio)-1-(pyrazol-4-yl)pyrrolidin-2-ones, 4-aryl-3-(arylthio)-4-chloro-N-(1-methylpyrazol-4-yl)butanamides, and tetrahydrofuran-2-iminium perchlorates which, when chromatographed, produce 5-aryl-4-(arylthio)dihydrofuran-2(3H)-ones and 4-aryl-3-(arylthio)-4-methoxy-N-(1-methyl-1H-pyrazol-4-yl)butanamides.     

CuSO4/sodium ascorbate catalysed synthesis of benzosuberone and 1,2,3-triazole conjugates: Design,synthesis and in vitro anti-proliferative activity

A novel series of conjugates of benzosuberone and 1,2,3-triazole i.e. 3-(4-phenyl-1H-1,2,3-triazol-1-yl)propyl-9-chloro-2,3-dimethyl-6,7-dihydro-5H-benzo[7]annulene-8-carboxylic acids (8a-j) were synthesized in good to excellent yields catalysed by CuSO₄ under milder reaction conditions and evaluated for their anti-proliferative activity. The structural elucidation of the prepared compounds was carried out using IR, ¹H NMR, ¹³C NMR and Mass spectral analysis. The newly synthesized derivatives (8a-j) were evaluated for their anti-proliferative activity against four human cell lines and the novel derivatives showed moderate to excellent activity. The obtained results suggest that these compounds can be considered as new hits for anti-proliferative drug development programme and further SAR studies can help obtain better anticancer agents.     

A simple method for extracting both active oily and water soluble extract (WSE) from Nigella sativa (L.) seeds using a single solvent system

The current study provides a way of extraction for both active NSO and WSE from Nigella sativa seeds using 98% methanol. About 1?kg of ground seeds was macerated by 1:2.5 w/v (g/mL) for 72?hours. After rotary evaporation and 7 days of continuous drying and chilling at 50 and 4?°C, NSO and WSE were obtained at the same instant. Solubility tests of 24 solvents and 11 thin layer chromatographic analyses while 2, 2-diphenyl-1-picrylhydrazyl free radical scavenging assay of NSO (73.66) , WSE (33.32) and NSO?+?WSE (78.22) against ascorbic acid (IC50?=?4.28?mg/mL) was performed. WSE was found to be highly soluble in water and 5% NaOH exhibiting the same Rf value of 0.95 for EtOH:DMSO (9:1) against the honey. WSE has revealed more than twofold higher anti-oxidant activity than others. Formulation of WSE with Tualang honey may provide better targeted hydrophilic drug delivery systems.     

Index for vehicle acoustical comfort inside a passenger car

Sound quality is among the main factors that influence customers’ preference for choosing good automobile products. It all started more than 10 years ago and grows up so fast due to high competition in the automotive industries. A-weighted noise levels and sound power are usually utilised to measure the noise but they are not adequate to characterise the impact sound inside a car. The most popular approach to determine sound quality of a product is to define an annoyance or specific index, which involves both subjective and objective evaluations. Subjective and objective tests should be studied concurrently in order to determine the sound quality inside a passenger car. This approach is used in this paper to evaluate vehicle comfort index according to most frequently used sound quality metrics, namely; Zwicker loudness, sharpness, roughness and fluctuation strength. As a result researchers of different fields of automotive acoustics investigations can use this index according to the type of road (international road roughness) without any need to perform time-consuming jury tests. The metrics are correlated with jury test results that show which of them and how much has affected the acoustical comfort of the vehicle. The relation between road roughness and vehicle acoustical comfort index is another point of interest in this research.     

Nanofluids thermal performance in the horizontal annular passages: a recent comprehensive review

Journal of Thermal Analysis and Calorimetry - Nanofluids are prepared to enrich thermo-physical and convective heat transfer properties by suspending nanometer particles in a base fluid. For...     

Validated LC–MS/MS method for quantitation of a selective JAK1 inhibitor,filgotinib in rat plasma,and its application to a pharmacokinetic study in rats

Filgotinib is a selective JAK1 (Janus kinase) inhibitor, filed in Japan for the treatment of rheumatoid arthritis. In this paper, we report a validated liquid chromatography coupled with tandem mass spectrometry for the quantification of filgotinib in rat plasma using tofacitinib as an internal standard (IS) as per the Food and Drug Administration regulatory guidelines. Filgotinib and the IS were extracted from rat plasma using ethyl acetate as an extraction solvent and chromatographed using an isocratic mobile phase (0.2% formic acid:acetonitrile; 20:80, v/v) at a flow rate of 0.9 mL/min on a Gemini C₁₈ column. Filgotinib and the IS were eluted at ~1.31 and 0.89 min, respectively. The MS/MS ion transitions monitored were m/z 426.3 → 291.3 and m/z 313.2 → 149.2 for filgotinib and the IS, respectively. The calibration range was 0.78–1924 ng/mL. No matrix effect and carryover were observed. Intra- and inter-day accuracies and precisions were within the acceptance range. Filgotinib was stable for three freeze–thaw cycles: on bench-top up to 6 h, in an autosampler up to 21 h, and at −80 ° C for 1 month. This novel method has been applied to a pharmacokinetic study in rats.     

Effects of polyvinylpyrrolidone on structural and optical properties of willemite semiconductor nanoparticles by polymer thermal treatment method

Journal of Thermal Analysis and Calorimetry - Willemite is an inorganic semiconductor material used for optoelectronic applications. The present study purposes a new polymer thermal treatment...     

Transverse conductivity in Pr_yY_{1-y}Ba_2Cu_3O_{7-\delta } single crystals in a wide range of praseodymium concentrations

A single-sized dielectric cylinder-based metamaterial is fabricated from TiO₂ nanoparticles, using a bottom-up approach. The sub-elements constituting the metalayer are embedded in a nonmagnetic transparent host matrix in the microwave regime and arranged in a square lattice. We demonstrate numerically and experimentally a broadband magnetic activity. The key feature to achieve this performance remains in the high aspect ratio of the metamaterial building blocks. This is a very promising step towards complex electromagnetic functions, involving low-cost metamaterials with simple fabrication.