Synthesis,Characterization, and Antimicrobial Activity of Carboxymethyl Chitosan-Graft-Poly(N-acryloyl,N′-cyanoacetohydrazide) Copolymers

Carboxymethyl chitosan was grafted with N-acryloyl,N′-cyanoacetohydrazide in homogenous aqueous phase using potassium persulfate initiator. The maximum grafting yield achieved was 448% at 0.03 mol/L potassium persulfate, 0.75 mol/L N-acryloyl,N′-cyanoacetohydrazide, and 60°C within 2 h. The grafted copolymers showed better thermal stability than that of carboxymethyl chitosan. The samples with percent grafting values up to 98% were soluble in water, but a higher grafting extent resulted in insoluble copolymers. The grafted copolymers are nontoxic materials and showed an inhibition effect on both Escherichia coli and Staphylococcus aureus bacteria and Aspergillus flavus and Candida albicans fungi better than those of chitosan and carboxymethyl chitosan themselves.     

Synthesis of some new pyrimidine derivatives and evaluation of their anticancer and antibacterial activities

Starting from the reaction of ethyl cyanoacetate with thiourea and the appropriate aldehydes, a series of new pyrimidine derivatives were prepared. Ten selected pyrimidine derivatives were subjected to a screening system for the investigation of their antitumor potency against liver (HEPG2) cell line. The antitumor activity results indicated that most of the selected pyrimidine derivatives showed moderate growth inhibition activity against the tested cell line, but with varying intensities in comparison to the known anticancer drugs: 5-fluorouracil and doxorubicin. Some of the synthesized compounds were also tested for their antimicrobial activity against bacteria as well as fungal isolates.     

Asymmetric aldol reactions catalyzed by the promiscuous aldo–ketoreductase enzyme

The promiscuous aldo–ketoreductase (AKR) enzyme is used as a sustainable biocatalyst for the first time to catalyze asymmetric aldol reactions in aqueous medium. The reactions between aromatic aldehydes and cyclic/acyclic ketones give the corresponding products in moderate yields and enantioselectivities in the presence of water. The influence of solvents, the mole ratio of substrates, and enzyme concentration are investigated. The mechanism of the AKR1A1-catalyzed aldol reaction is also discussed.     

Preparation and Characterization of Modified Cellulose Adsorbents with High Surface Area and High Adsorption Affinity for Hg(II)

Cellulose was modified via chlorination using phosphorous oxychloride followed by functionalization with amine and thiol moieties. The obtained modified cellulose samples were investigated by means of FTIR, TGA, TEM, and nitrogen-adsorption surface area (BET). The BET measurements showed a remarkable increase in the surface area of Cell-N-S (477.7 m²/g) and Cell-N (706 m²/g). The resins gave an uptake capacities of 38 and 7.2mmol/g for Cell-N-S and Cell-N, respectively toward Hg(II) from its solutions. These values are considered much better compared with other reported resins. Regeneration of the resins was achieved effectively using acidified thiourea.     

Efficient Catalytic and Thermal Syntheses of Novel Thiadiazole,Triazole, Benzothiazole,and Fused Quinazoline Derivatives

Russian Journal of Organic Chemistry - A thiourea derivative, 4-chloro-N-[(4-chlorophenyl)carbamothioyl]benzamide, was oxidized with iodine in acetic acid to give the corresponding disulfide,...     

Adsorption of cationic methylene blue dye using microwave-assisted activated carbon derived from acacia wood: Optimization and batch studies

This study assesses the performance of optimized acacia wood-based activated carbon (AWAC) as an adsorbent for methylene blue (MB) dye removal in aqueous solution. AWAC was prepared via a physicochemical activation process that consists of potassium hydroxide (KOH) treatment, followed by carbon dioxide (CO₂) gasification under microwave heating. By using response surface methodology (RSM), the optimum preparation conditions of radiation power, radiation time, and KOH-impregnation ratio (IR) were determined to be 360 W, 4.50 min, and 0.90 g/g respectively, which resulted in 81.20 mg/g of MB dye removal and 27.96% of AWAC’s yield. Radiation power and IR had a major effect on MB dye removal while radiation power and radiation time caused the greatest impact on AWAC’s yield. BET surface area, mesopore surface area, and pore volume of optimized AWAC were found to be 1045.56 m²/g, 689.77 m²/g, and 0.54 cm³/g, respectively. Adsorption of MB onto AWAC followed Langmuir and pseudo-second order for isotherm and kinetic studies respectively, with a Langmuir monolayer adsorption capacity of 338.29 mg/g. Mechanism studies revealed that the adsorption process was controlled by film diffusion mechanism and indicated to be thermodynamically exothermic in nature.     

Discovery of New Coumarin-Based Lead with Potential Anticancer,CDK4 Inhibition and Selective Radiotheranostic Effect: Synthesis, 2D & 3D QSAR,Molecular Dynamics,In Vitro Cytotoxicity,Radioiodination, and Biodistribution Studies

Novel 6-bromo-coumarin-ethylidene-hydrazonyl-thiazolyl and 6-bromo-coumarin-thiazolyl-based derivatives were synthesized. A quantitative structure activity relationship (QSAR) model with high predictive power r² = 0.92, and RMSE = 0.44 predicted five compounds; 2b, 3b, 5a, 9a and 9i to have potential anticancer activities. Compound 2b achieved the best ΔG of –15.34 kcal/mol with an affinity of 40.05 pki. In a molecular dynamic study 2b showed an equilibrium at 0.8 Å after 3.5 ns, while flavopiridol did so at 0.5 Å after the same time (3.5 ns). 2b showed an IC₅₀ of 0.0136 µM, 0.015 µM, and 0.054 µM against MCF-7, A-549, and CHO-K1 cell lines, respectively. The CDK4 enzyme assay revealed the significant CDK4 inhibitory activity of compound 2b with IC₅₀ of 0.036 µM. The selectivity of the newly discovered lead compound 2b toward localization in tumor cells was confirmed by a radioiodination biological assay that was done via electrophilic substitution reaction utilizing the oxidative effect of chloramine-t. ¹³¹I-2b showed good in vitro stability up to 4 h. In solid tumor bearing mice, the values of tumor uptake reached a height of 5.97 ± 0.82%ID/g at 60 min p.i. ¹³¹I-2b can be considered as a selective radiotheranostic agent for solid tumors with promising anticancer activity.     

Bioactive Components of Salvia and Their Potential Antidiabetic Properties: A Review

The utilization of therapeutic plants is expanding around the globe, coupled with the tremendous expansion of alternative medicine and growing demand in health treatment. Plants are applied in pharmaceuticals to preserve and expand health—physically, mentally and as well as to treat particular health conditions and afflictions. There are more than 600 families of plants identified so far. Among the plants that are often studied for their health benefit include the genus of Salvia in the mint family, Lamiaceae. This review aims to determine the bioactive components of Salvia and their potential as antidiabetic agents. The search was conducted using three databases (PubMed, EMBASE and Scopus), and all relevant articles that are freely available in the English language were extracted within 10 years (2011–2021). Salvia spp. comprises many biologically active components that can be divided into monoterpenes, diterpenes, triterpenes, and phenolic components, but only a few of these have been studied in-depth for their health benefit claims. The most commonly studied bioactive component was salvianolic acids. Interestingly, S. miltiorrhiza is undoubtedly the most widely studied Salvia species in terms of its effectiveness as an antidiabetic agent. In conclusion, we hope that this review stimulates more studies on bioactive components from medicinal plants, not only on their potential as antidiabetic agents but also for other possible health benefits.     

Facile synthesis and antimicrobial evaluations of some novel pyrazolo[3,4-b]selenolo[3,2-e]pyrazines and their related heterocycles

A new series of pyrazolopyrazinoselenolotriazolopyrimidines was synthesized by a facile method based on condensation of 5-amino-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]selenolo[3,2-e]pyrazine-6-carbonitrile ( 3 ) with triethyl orthoformate followed by intramolecular cyclization with hydrazine to afford 7-amino-8-imino-3-methyl-1-phenyl-1,8-dihydro-7H-pyrazolo[3″,4″:5′,6′]pyrazino[2′,3′:4,5] selenolo[3,2-d]pyrimidine ( 5 ). The latter compound was utilized as a multipurpose precursor for the construction of other new triazoles fused to the pyrazolopyrazino- selenolopyrimidine moiety. Alternatively, acetylation and chloro-acetylation of compound 3 using acetic anhydride and chloroacetyl chloride yielded the acetyl amino 11 and chloroacetamido 12 derivatives, respectively. Compound 12 underwent nucleophilic substitution upon reaction with morpholine to provide the morpholinyl acetamide 13 . Furthermore, the pyrazolopyridoselenolopyrazine ring system 14 was synthesized by the reaction of the o-amino-carbonitrile 3 with malononitrile. Assignment of the chemical structures for the new compounds was confirmed depending on elemental and spectral techniques. On the other hand, most of the synthesized compounds revealed promising results against various bacterial and fungal strains.     

Gel-assisted synthesis of anatase TiO2 nanoparticles and application for electrochemical determination of L-tryptophan

Anatase titanium dioxide nanoparticles (TiO₂-NPs) were synthesized with and without gelatin via the sol-gel method. The TiO₂-NPs were characterized by a number of techniques, such as thermogravimetric analysis (TGA), X-ray diffraction analysis (XRD), transmission electron microscopy (TEM), fourier transform infrared spectroscopy (FT-IR) and ultraviolet visible spectroscopy (UV-Vis). The particle sizes of the TiO₂-NPs prepared with and without gelatin were ～13 and ～17 nm, respectively. The main advantage of using gelatin as a stabilizing agent is that it provides long-term stability for nanoparticles by preventing particles agglomeration. The results indicated that gelatin was a reliable green stabilizer, which can be used as a polymerization agent in the sol-gel method for synthesis of tiny size TiO₂-NPs. Moreover, the composite film was prepared by synthesized TiO₂-NPs nanoparticles and multi wall carbon nanotube (MWNT) on glassy carbon electrode (TiO₂-MWNT/GCE). The TiO₂-MWNT/GCE responded linearly to L-tryptophan (L-Trp) in the concentration of 1.0 × 10^?6 to 1.5 × 10^?4 M with detection limit of 5.2 × 10^?7 M at 3 using amperometry. The studied sensor exhibited good reproducibility and long-term stability.