Pyridylethylation - a new protection method for active hydrogen compounds

2-(2- or 4-Pyridyl)ethyl group is readily introduced by pyridylethylation and easily removed after activation by quaternisation with methyl iodide.     

Radiolabeling of anti-carcinoembryonic antigen (CEA) monoclonal antibody (MAb BW 431/26) for clinical applications

A method for labeling of anti-carcinoembryonic antigen (CEA) monoclonal antibody (MAb) BW 431/26 is described. For preparations of^99mTc-anti-CEA complex, a solution (1 ml) of tetrasodium-1,1,3,3-propanetetetraphosphate dihydrate (2.7 mg), stannous chloride dihydrate (0.12 mg) and sodium chloride (0.2 mg) in 5 ml of 0.9% saline was added to a vial containing monoclonal antibody (2 mg) from mouse (MAb BW 431/26), D-glucitol (2 mg) and sodium sulfate (2 mg) to obtain a clear solution. A quantitative labeling yield of the MAb BW 431/26 was achieved by addition of 5 ml (40.5 mCi, 1.5 Gbq) technetium-99m-pertechnetate (^99mTcO₄) generator eluate at room temperature within 10 minutes. The radiochemical purity determined by ITLC (Gelman, SG) plates was >95%.     

Nitriles with High Gas-Phase Basicity—Part II Transmission of the Push–Pull Effect through Methylenecyclopropene and Cyclopropenimine Scaffolds Intercalated between Different Electron Donor(s) and the Cyano N-Protonation Site

This work extends our earlier quantum chemical studies on the gas-phase basicity of very strong N-bases to two series of nitriles containing the methylenecyclopropene and cyclopropenimine scaffolds with dissymmetrical substitution by one or two electron-donating substituents such as Me, NR₂, N=C (NR₂)₂, and N=P (NR₂)₃, the last three being strong donors. For a proper prediction of their gas-phase base properties, all potential isomeric phenomena and reasonable potential protonation sites are considered to avoid possible inconsistencies when evaluating the energetic parameters and associated protonation or deprotonation equilibria B + H⁺ = BH⁺. More than 250 new isomeric structures for neutral and protonated forms are analyzed. The stable structures are selected and the favored ones identified. The microscopic (kinetic) gas-phase basicity parameters (PA and GB) corresponding to N sites (cyano and imino in the cyclopropenimine or in the substituents) in each isomer are calculated. The macroscopic (thermodynamic) PAs and GBs, referring to the isomeric mixtures of favored isomers, are also estimated. The total (pushing) substituent effects are analyzed for monosubstituted and disubstituted derivatives containing two identical or two different substituents. Electron delocalization is examined in the two π–π conjugated transmitters, the methylenecyclopropene and cyclopropenimine scaffolds. The aromatic character of the three-membered ring is also discussed.     

Highly active sites of NiVB nanoparticles dispersed onto graphene nanosheets towards efficient and pH-universal overall water splitting

Production of hydrogen (H2) and oxygen (O2) through electrocatalytic water splitting is one of the sustainable,green and pivotal ways to accomplish the ever-inc...     

In Vitro and In Vivo Anti-Arthritic Potential of Caralluma tuberculata N. E. Brown. and Its Chemical Characterization

Present research was planned to assess the in vitro and in vivo anti-arthritic potential of Caralluma tuberculata N. E. Brown. methanolic (CTME) and aqueous (CTAQ) extracts. Chemical characterization was done by high-performance liquid chromatography and gas chromatography–mass spectrometry analysis. The Complete Freund’s Adjuvant (CFA) was injected in left hind paw of rat at day 1 and dosing at 150, 300 and 600 mg/kg was started on the 8th day via oral gavage in all groups except normal and disease control rats (which were given distilled water), whereas methotrexate (intraperitoneal; 1 mg/kg/mL) was administered to standard control. The CTME and CTAQ exerted significant (p < 0.01–0.0001) in vitro anti-arthritic action. Both extracts notably reduced paw edema, and restored weight loss, immune organs weight, arthritic score, RBCs, ESR, platelet count, rheumatoid factor (RF), C-reactive protein, and WBCs in treated rats. The plant extracts showed significant (p < 0.05–0.0001) downregulation of tumor necrosis factor-α, Interleukin-6, -1β, NF-κB, and cyclooxygenase-2, while notably upregulated IL-4, IL-10, I-κBα in contrast to disease control rats. The plant extracts noticeably (p < 0.001–0.0001) restored the superoxide dismutase and catalase activities and MDA levels in treated rats. Both extracts exhibited significant anti-arthritic potential. The promising potential was exhibited by both extracts probably due to phenolic, and flavonoids compounds.     

Recent trends in the chemistry of Sandmeyer reaction: a review

Metal-catalyzed reactions play a vital part to construct a variety of pharmaceutically important scaffolds from past few decades. To carry out these reactions under mild conditions with low-cost easily available precursors, various new methodologies have been reported day by day. Sandmeyer reaction is one of these, first discovered by Sandmeyer in 1884. It is a well-known reaction mainly used for the conversion of an aryl amine to an aryl halide in the presence of Cu(I) halide via formation of diazonium salt intermediate. This reaction can be processed with or without copper catalysts for the formation of C–X (X?=?Cl, Br, I, etc.), C-CF₃/CF₂, C–CN, C–S, etc., linkages. As a result, corresponding aryl halides, trifluoromethylated compounds, aryl nitriles and aryl thioethers can be obtained which are effectively used for the construction of biologically active compounds. This review article discloses various literature reports about Sandmeyer-related transformations developed during 2000–2021 which give different ideas to synthetic chemists about further development of new and efficient protocols for Sandmeyer reaction.

Graphical abstract

An updated compilation of new approaches for Sandmeyer reaction is described in this review to construct a variety of carbon-halogen, carbon-phosphorous, carbon-sulfur, carbon-boron etc. linkages.

     

Weak deflection angle and shadow cast by the charged-Kiselev black hole with cloud of strings in plasma

In this study, the gravitational deflection angle of photons in the weak field limit (or the weak deflection angle) and shadow cast by the electrically charged and spherically symmetric static Kiselev black hole (BH) in the string cloud background are investigated. The influences of the BH charge Q, quintessence parameter γ, and string cloud parameter a on the weak deflection angle are studied using the Gauss-Bonnet theorem, in addition to studying the influences on the radius of photon spheres and size of the BH shadow in the spacetime geometry of the charged-Kiselev BH in string clouds. Moreover, we study the effects of plasma (uniform and non-uniform) on the weak deflection angle and shadow cast by the charged-Kiselev BH surrounded by the clouds of strings. In the presence of a uniform/nonuniform plasma medium, an increase in the string cloud parameter a increases the deflection angle α. In contrast, a decrease in the BH charge Q decreases the deflection angle. Further, we observe that an increase in the BH charge Q causes a decrease in the size of the shadow of the BH. We notice that, with an increase in the values of the parameters γ and a, the size of the BH shadow increases, and therefore, the intensity of the gravitational field around the charged-Kiselev BH in string clouds increases. Thus, the gravitational field of the charged-Kiselev BH in the string cloud background is stronger than the field produced by the pure Reissner-Nordstrom BH. Moreover, we use the data released by the Event Horizon Telescope (EHT) collaboration, for the supermassive BHs M87* and Sgr A*, to obtain constraints on the values of the parameters γ and a.     

Mixed micellization and interfacial properties of dodecyltrimethylammonium bromide and tetraethyleneglycol mono-n-dodecyl ether in absence and presence of sodium propionate

Mixed micelle formation and interfacial properties of aqueous binary surfactant combinations of dodecyltrimethylammonium bromide (C12TAB) and tetraethyleneglycol mono-n-dodecyl ether (C12E4) at 30 degrees C in absence and presence of sodium propionate (NaPr) have been investigated. The critical micelle concentration, aggregation number, micropolarity and interfacial adsorption have been quantitatively estimated by surface tension and steady-state fluorescence measurements. The micellar and adsorption characteristics like composition, activity coefficients and mutual interaction parameters have been estimated following different theoretical treatments like that of Clint, Rubingh, Rodenas, Maeda, Blankschtein and Rosen. The analysis reveals very small mole fraction of cationic surfactant in both the mixed micelles and mixed monolayer inspite of synergism. Blankschtein's model predicts a continuous decrease in synergism due to the salt effect of NaPr; Rubingh's approach, on the contrary, indicates an increase in it above 30 mM of NaPr concentration. Aggregation number variation with NaPr indicates the same. Mixed monolayer shows better synergism compared to that in mixed micelles which increases with the addition of sodium propionate above 30 mM concentration.