Russian Journal of General Chemistry最新文献

Inclusion compounds of diclofenac sodium, a non-steroidal anti-inflammatory drug, with native α-, β- and γ-cyclodextrins at varying levels of hydration were prepared by co-grinding in a ball mill. Using TG/DSC analysis, powder X-ray diffraction and solid-state IR spectroscopy, it was shown that when equimolar mixtures of native cyclodextrin and diclofenac are milled, complete inclusion of this pharmaceutical ingredient occurs, regardless of cyclodextrin hydration. The absence of water-guest competition in the solid-state inclusion process is explained by high affinity of diclofenac sodium to cyclodextrins. The prepared complexes have a significantly lower thermal stability than the separate native cyclodextrins and diclofenac sodium.

3-[5-(Cycloheximino)-4,5-dihydro-1,3,4-thiadiazol-2-yl]pyridine-2-amine was synthesized and used to make a novel pyrazole derivative embedded polymer inclusion membrane (Py@PIM). The surface and structure morphology of Py@PIM was detected using thermogravimetric analysis, FT-IR spectroscopy and scanning electron microscopy. Donnan dialysis system was also used to assess the transport efficacy of Py@PIM towards 5 heavy metals (Co, Cd, Cu, Ni, Pb). The results show that according to the kinetic coefficient, the order is Pb > Ni > Co > Cd > Cu. Similar kinetic order was also observed in multiple cation experiments, in experiments where all cations were mixed in a single cell.

An efficient one-pot approach was proposed for the synthesis of novel sulfonyl-1H-1,2,3-triazolo-1H-imidazole-2-sulfonamides. The newly synthesized derivatives were screened for in vitro antibacterial inhibition potency against gram-positive strains. Among the tested compounds, N-({1-[(4-chlorophenyl)sulfonyl]-1H-1,2,3-triazol-4-yl}methyl)-1-methyl-1H-imidazole-2-sulfonamide and N-({1-[(4-cyanophenyl)sulfonyl]-1H-1,2,3-triazol-4-yl}methyl)-1-methyl-1H-imidazole-2-sulfonamide had a minimum inhibitory concentration (MIC) of 3.12 μg/mL against B. subtilis, which is two times higher than the normal streptomycin (6.25 μg/mL). It also had a MIC value of 6.25 μg/mL against S. aureus that was the same as the positive control. Also the antibiofilm profiles for the potent compounds showed that the active derivatives were not only very good at killing bacteria, but they were also very good at stopping the growth of B. subtilis biofilm.

1,8-Diazabicyclo[5.4.0]undec-7-ene (DBU) was used as a mild and efficient catalyst for synthesis of various dihydropyrano[3,2-c]chromene-3-carboxylate derivatives via one-pot, three-component condensation of aromatic aldehydes, active methylene and 4-hydroxycoumarin in ethanol under reflux. The distinctive features of this process are mild reaction conditions, reusability of the reaction media, short reaction time, easy isolation of products and good yield. In addition, the effect of electron donating and withdrawing groups on the reactivity of chromene derivatives was investigated and evaluated by quantum chemical tools. For this purpose, the FMO analyses were performed and considered in terms of the new perspectives of the C-DFT. Also, the NBO analyses of the chromene derivatives were conducted to look for and compare the resonance and inductive effect on the possible reactivity behaviors.

Tuberculosis (TB), which has been a scourge of humanity for thousands of years, is a worldwide pandemic disease caused mainly by M. tuberculosis (Mtb). The appearance of TB and the emergence of drug resistance (DR) requires focused attention and the need to approve the various isoniazid (INH) analogs. The DR-TB, multidrug resistance (MDR), extensively drug-resistant (XDR), and totally drug-resistant (TDR) TB increase the challenges to eliminate TB globally. INH is an important heterocyclic moiety in medicinal chemistry due to the presence of an active site, which extends its applications and is a frontline key anti-TB drug. In this review, we aim to summarize synthetic strategies and pharmacological properties of INH analogs and we also discussed INH analogs as potent anti-TB agents. This review summarized the recent advances of anti-TB agents holding INH as a nucleus. Data on collection of various INH analogs and their biological activities like anti-TB, antibacterial, antifungal, antiviral, etc. were presented.

The review considers new quaternary ammonium compounds based on pyridoxine derivatives, which were obtained and studied in 2013–2023 at the Research and Educational Center for Pharmacy of the Kazan (Volga Region) Federal University. Four structurally related classes of compounds are discussed, including mono- and bis-ammonium derivatives of pyridoxine, pyridoxine derivatives with cleavable linkers bearing an ammonium moiety, and ammonium derivatives of the unnatural pyridoxine mimetic, 3-hydroxypyridine. Synthetic schemes, biological properties, and key structure–activity relationships of the target structural series are described. For the lead-compounds belonging to specific structural chemotypes, a comprehensive profile of pharmacological properties is described, including antibacterial activity against a wide panel of Gram-positive and Gram-negative bacterial strains including clinical isolates; in vitro and in vivo toxicity; influence on the development of drug resistance. The mechanisms of action of the considered compounds as well as the prospects for their practical use are discussed.

New methods for the direct preparation of 3-hydroxy-1-adamantanecarboxylic acid and 1,3-adamantanedicarboxylic acid from 1-adamantyl halides was developed. The one-pot methods are based on the sequential combination of the Koch–Haaf and oxidation reactions in a H₂SO₄–HNO₃ mixture. This study proposes an improved method for the preparation of 1-adamantanecarboxylic acids from 1-adamantyl halides.

The application of lightweight carbon materials and their composites in solid propellants, especially graphene and its derivatives as combustion catalysts in the combustion performance regulation of propellants have attracted attention in the field of aerospace propulsion. The energetic composite µAl/NGO was prepared using nitrated graphene oxide (NGO) and micron-aluminum powder (µAl) as raw materials by solution method. The structure and morphology of the composite was characterized by elemental analysis, Fourier-transform infrared spectroscopy, X-ray diffraction, X-ray photoelectron spectroscopy and scanning electron microscopy. The thermal properties of the composite were analyzed by TG-DSC test results. The results show that µAl is uniformly distributed on the surface of NGO, and the crystal structure of µAl is not changed. In the temperature range of 300–450°C, µAl/NGO explodes, and it is a rapid exothermic reaction with a peak temperature of 364°C. In this temperature range, the decomposition of NGO and the oxidation of µAl occurred simultaneously by TG results. Compared with the enthalpy of oxidation exothermic process of the pure µAl at 557°C (2274 J/g), the enthalpy of decomposition and oxidation exothermic processes of µAl/NGO is increased to 10484 J/g, which is nearly 5 times higher than that of the pure µAl. The result of μAl/NGO catalytic behavior on the thermal decomposition of ammonium perchlorate (AP) indicate that μAl/NGO has little effect on the low temperature thermal decomposition of AP, but the peak of high temperature thermal decomposition advances from 404 to 364°C. The kinetic analysis results show that the activation energy of the high-temperature exothermic reaction of AP is increased by nearly 100 kJ/mol.

New phosphorus-containing isatin-3-hydrazones were synthesized by the condensation reaction of 5-substituted isatins with 2-chloroethyl [4-(dimethylamino)phenyl](2-hydrazinyl-2-oxoethyl)phosphinate (KAPAKh). The resulting compounds were shown to have high antitumor activity against duodenal adenocarcinoma (HuTu80) and cervical epithelioid carcinoma (M-HeLa) cell lines with low toxicity towards erythrocytes and normal human liver cells.

TiO₂ nanoparticles (TiO₂NPs) were prepared using the Carchorus hirsutus plant leaf extract and investigated for biomedical applications. The synthesized TiO₂NPs were characterized by UV-visible, FTIR, XRD, SEM, EDS, and TEM methods and tested for haemolytic activity. The anticancer activity was investigated using MCF7 and HeLa cell lines. The antimicrobial activity was tested against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Salmonella typhi and Candida albicans.