Russian Journal of Organic Chemistry最新文献

Bis-1,3,4-oxadiazoles and bis-1,3,4-thiadiazoles with aryl and alkyl linkers have been synthesized. The pharmacophore electron-deficient groups (carboxylic, nitrile) have been introduced into the molecule to increase their hydrophilicity and potential biological activity. Functionalized compounds have demonstrated a new type of biological activity, i.e., inhibition of lipid oxidation revealed as a decrease in the amount of MDA.

A new method for the synthesis of a bisbenzylisoquinoline base with a diphenyl oxide fragment based on phosphorane obtained from N-homoveratrylmaleimide has been suggested.

Here in this article we described the synthesis of 5-benzylidene-2-thioxothiazolidin-4-one derivative via one pot reaction mechanism with excellent yield in short reaction time using conventional and microwave irradiation methods. Lemon juice used as a green solvent, ammonium ferrous sulfate as catalyst in the presence of sodium citrate buffer as base reduces the time cycle and increased the yields. In addition, screening of various metal catalysts was studied. This methodology gave excellent yield and purity as compared with earlier reported process. The advantages of this process are cost-effective, short reaction time, high atom economy and environmental friendly. In addition, as compared to traditional heating approach, the microwave-assisted synthesis offered outstanding yields.

Interaction of 1-phenyl-4,6-dimethylpyrimidine-2(1H)-one with 4-mercaptobuturic acid hydrazide proceeds as ANRORC (Addition of the Nucleophile–Ring Opening–Ring Closure) process and results in the formation with 60% yield of 1-(4-mercaptobutanoyl)-3,5-dimethyl-5-(3-phenylcarbamoylamino)-2-pyrazoline as promising сo-ligand for the preparation of gold glyco-nanoparticles for biomedical purposes.

–The parent nuclear structure of piperine served as the basis for the design and synthesis of thirteen derivatives through nucleophilic substitution method. These derivatives were subsequently characterized by ¹H NMR, ¹³C NMR, and HR-MS analysis. The antiproliferative activities of these compounds against 293T human normal cells, as well as MDA-MB-231 (breast) and Hela (cervical) cancer cell lines were assessed through the MTT assay. Compound 4b exhibited remarkable antiproliferative activity against Hela cells (IC₅₀ = 1.80 μM), surpassing that of both 5-fluorouracil (IC₅₀ = 44.58 μM) and piperine itself. Furthermore, subsequent investigations revealed that compound 4b displayed significant anti-proliferation, anti-migration and anti-invasion effects on Hela cells. These findings suggest that compound 4b may be a promising lead compound for the treatment of cervical carcinoma.

2-{[(2Z)-4-Aryl-2-hydroxy-4-oxobut-2-enoyl]amino}benzoic acids have been synthesized through the reaction of methyl esters of aroylpyrovinic acids with 2-aminobenzoic (anthranilic) acid in glacial acetic acid in the presence of anhydrous sodium acetate. The spatial structure of the compounds has been confirmed using X-ray crystallography.

In the present work, the aryl-substituted pyrazolone derivative ethyl 3-((3-methyl-1-phenyl-1H-pyrazol-5-yl)oxy)-2-methyleneheptanoate (ETT) has been synthesized by the reaction of Baylis-Hillman acetate with pyrazolones and screened for their in vitro antifungal, antibacterial, and antioxidant properties. The molecule shows good in vitro antifungal and antibacterial activities due to the presence of pentane, which enhances the absorption rate by its increased lipid solubility and improves the pharmacological activity. It is also evident from the results obtained from structure-activity relationship (SAR) studies. In silico studies were conducted on the synthesized molecule, examining its interactions with DNA Gyrase, Lanosterol14 alpha demethylase, and KEAP1-NRF2 proteins. The results revealed strong binding interactions at specific sites. Further, the photophysical properties of synthesized compounds were theoretically estimated using the ab-intio technique. The ground state optimization, dipole moment, and HOMO–LUMO energy levels are calculated using the DFT-B3LYP-6-31G(d) basis set. Using the theoretically estimated HOMO–LUMO value, global chemical reactivity descriptor parameters are estimated, and the result shows the synthesised molecule has a highly electronegative and electrophilic index. NBO analysis proved the presence of intermolecular ON^.H hydrogen bonds caused by the interaction of the lone pair of oxygen with the anti-bonding orbital. The results suggest that pentane-substituted pyrazolone derivatives show good photophysical and biological applications.

The green synthesis of silver and copper nanoparticles using Solanum trilobatum root extract as a capping representative. These studies changed into excited up at the synthesis of nanoparticles to offer paintings for two exclusive metals (silver nitrate and copper sulfate) with the aid of using the use of Solanum trilobatum root. We did a comparative study of synthesized silver and copper nanoparticles using about 10 g of Solanum trilobatum root was weighed separately and transferred into 250 mL beakers containing 100 mL distilled water and boiled for about 25 min solutions were then filtered to get clear extracts. The extract was taken for the reduction of Ag⁺ and Cu²⁺ ions, and 10 mL of Solanum trilobatum root extract was added drop wise to 10 mL of silver nitrate and copper sulfate solution (1 : 1 ratio). The UV-visible spectroscopy is a commonly used technique. Light wavelengths in the 300–800 nm are generally used for characterizing colorful essence nanoparticles in the size range of 2 to 100 nm. Spectrophotometric absorption measurements in the wavelength ranges of 400–450 and 500–550 nm are used in characterizing the silver and copper nanoparticles, respectively. FT-IR spectroscopy is useful for characterizing surface chemistry. Organic functional groups (carbonyls, hydroxyls) attached to the face of nanoparticles and the other face chemical remainders are detected using FT-IR. Scanning electron microscope and transmission electron microscopy are used for morphological characterization at the nanometer to micrometer scale. Transmission electron microscopy has a 1000-fold higher resolution compared with scanning electron microscope.

The 1,3-dipolar cycloaddition reaction of substituted dinitroacetonitriles with isoquinoline in the presence of acetylene dicarboxylic acid dimethyl ester results in the formation of a mixture of diastereomeric dimethyl 2-dinitromethyl-1,1bH-pyrimido[2,1-a]isoquinoline-3,4-dicarboxylates. The obtained compounds can be considered as promising synthons with potential antituberculosis and fungicidal activity.