Synthesis of Derivatives of 2,6-Dideoxy-2,2-Difluoro-3-O-Methyl-l-Arabinopyranose (2,2-Difluorooleandrose)

Abstract

L-Oleandrose is the carbohydrate constituent of the potent anthelmintic agents the avermectins. Diethylaminosulfur tri-fluoride treatment of appropriate uloses did not give gem-difluoro sugars. Trifluorofluoroxymethane or xenon difluoride addition to the double bond of 4-O-benzoyl-6-deoxy-2-fluoro-3-O-methyl-L-glucal produced protected 2,2-difluorooleandrose derivatives activated at their anomeric center and ready for glycosidation.     

Intramolecular aglycon delivery for (1 → 2)-β-mannosylation: towards the synthesis of phospholipomannan of Candida albicans

A high yielding method for 1,2-cis-β-D-mannosylation by intra-molecular aglycon delivery (IAD) through p-methoxy benzyl ether/acetal exchange and phenylsulfoxide donor is reported, along with its application in iterative assembly of antigenic (1 → 2)-β-pentamannoside domain of phospholipomannan (PLM) of fungal pathogen Candida albicans.     

An efficient ‘on-water’ synthesis of 1,4-dihydropyridines using Fe3O4@SiO2 nanoparticles as a reusable catalyst

An ‘on-water’, efficient, high yielding, expeditious method has been developed for the synthesis of 1,4-dihydropyridine (1,4-DHP) derivatives via an one-pot multi-component condensation of dimedone or 4-hydroxycoumarine, aldehydes, and ammonium acetate using Fe₃O₄@SiO₂ nanoparticles as a recyclable heterogeneous catalyst. This method takes advantage of the fact that water, a green solvent is used in combination with Fe₃O₄@SiO₂ nanoparticles as catalyst which can be easily recovered magnetically and reused for further runs.     

Poly-hydroxamic acid (PHA) matrix for gadolinium pre-concentration and removal

A novel hydrophilic, three dimensionally cross-linked, aliphatic backbones with pendant hydroxamic acid (HA) group as functional moiety has been synthesized and utilized targeting removal of gadolinium [Gd(III)] from laboratory waste aqueous effluent. To understand the nature of sorption, gadolinium solution of various concentrations viz., 20, 10, 5.0, 1.0, 0.5 and 0.1 ppm has been contacted with a dose rate of 1 g/100 mL for 2 h. In this study, ICP-AES has been used for determination of concentration (ppm) of gadolinium in feed, filtrate and elute. EDXRF study also ensures the presence of gadolinium in the respective medium. Loaded gadolinium matrix was eluted with 1 N HCl for determining the elution factor (0.98).     

Brief survey on phytochemicals to prevent COVID-19

BackgroundThe recent pandemic by COVID-19 is a global threat to human health. The disease is caused by SARS-CoV-2 and the infection rate is increased more quickly than MERS and SARS as their rapid adaptation to varied climatic conditions through rapid mutations. It becomes more severe due to the lack of proper therapeutic drugs, insufficient diagnostic tool, scarcity of appropriate drug, life supporting medical facility and mostly lack of awareness. Therefore, preventive measure is one of the important strategies to control. In this context, herbal medicinal plants received a noticeable attention to treat COVID-19 in Indian subcontinent. Here, 44 Indian traditional plants have been discussed with their novel phytochemicals that prevent the novel corona virus. The basic of SARS-CoV-2, their common way of transmission including their effect on immune and nervous system have been discussed. We have analysed their mechanism of action against COVID-19 following in-silico analysis. Their probable mechanism and therapeutic approaches behind the activity of phytochemicals to stimulate immune response as well as inhibition of viral multiplication discussed rationally. Thus, mixtures of active secondary metabolites/phytochemicals are the only choice to prevent the disease in countries where vaccination will take long time due to overcrowded population density.     

Charge screening in a plasma with an external ionization source

An asymptotic theory for the screening of the electric field of a dust particle or a spherical probe in a plasma with an external steady and/or internal (proportional to the electron density) gas ionization source has been developed for the first time. It has been established that the screening of the charge of a spherical body adsorbing the charge of the incident plasma particles is described by a superposition of two exponentials with different screening constants. The two exponentials are retained even in the absence of nonequilibrium fluxes on the macroparticle and only in the special case of an isothermal plasma does the screening become Debye one. The screening length is determined by the ratio of the electron-ion, β_ei, and Langevin, β_L = 4πeμ_i (where μ_i is the ion mobility), recombination coefficients. If β_L ? β_ei, then it is much larger than the electron Debye length. The ions in an isothermal plasma have been found to give the same contribution to the screening as the electrons if the electron-ion recombination coefficient exceeds the Langevin ion recombination coefficient by a factor of 2 or more, β_ei ≥ 2β_L. The Vlasov equation is used to analyze the asymptotic behavior of the macroparticle potential in a collisionless plasma.     

Synthesis and Biological Studies of O3-Aryl Galactosides as Galectin Inhibitors

β-Galactose derivatives have recently been reported to selectively inhibit galectin-3, and a library of O3-arylated galactosides with varying substitution patterns was designed to study such inhibitions further. The O3-arylated galactosides were synthesized using diaryliodonium salts under mild and transition metal free conditions, providing the target products in moderate to good yields. An O3-trifluoroethylated galactoside was also synthesized using iodonium salt chemistry. Azido-substituted products were subsequently transformed into the corresponding triazoles. After deprotection, a selection of galactoside derivatives were evaluated for inhibitory potencies against galectins-1, 3, 4 N (N-terminal domain), 4 C (C-terminal domain), 7, 8 N, 8 C, 9 N, and 9 C and one compound with promising affinity and selectivity for both the N- and C-terminal domain of galectin-9 was discovered.