Synthesis of spirooxindolocarbamates based on Betti reaction: antibacterial,antifungal and antioxidant activities

Molecular Diversity - A series of new spirooxindolocarbamates 4a–l and 6a–d were synthesized by using the Betti reaction. All the target compounds were well characterized by IR, NMR and...     

Ultrasound mediation for one-pot multi-component synthesis of amidoalkyl naphthols using new magnetic nanoparticles modified by ionic liquids

The ionic liquid 1-methyl-3-(3-trimethoxysilylpropyl) imidazolium acetate was immobilized on the Fe₃O₄ nanoparticles (MNPs-IL-OAc) and used as an efficient new heterogeneous nanocatalyst for the one-pot multi-component synthesis of 1-amidoalkyl-2-naphthols under ultrasound irradiation. The advantages of present combined method are the use of a low scale catalyst, easier work-up procedure, waste-free, green and efficient synthetic entry to excellent yield of products in a high reusability and a short reaction time.     

One-step synthesis of silver nanoparticles in an aqueous solution and their antibacterial activities

A one-step simple synthesis of silver colloid nanoparticles with controllable sizes is presented in this research. In the synthesis, an amino-terminated hyperbranched polymer (HBP-NH₂) was applied as a stabilizer and a reductant. The syntheses, performed at various initial AgNO₃ concentrations (0.28–0.56 g/l) in a 2 g/l HBP-NH₂ aqueous solution, produced silver colloid nanoparticles having average sizes from 3 to 30 nm with narrow size distributions. The formation of silver colloid nanoparticles was characterized by Fourier Transform Infrared Spectrophotometry (FTIR), Dynamic Light Scattering (DLS), Transmission Electron Microscopy (TEM), UV/Visible Absorption Spectrophotometry, and X-ray Diffraction (XRD) measurements. The results indicated that both particle size and the UV absorption are strongly dependent on the initial AgNO₃ concentrations. The silver colloid nanoparticles, prepared with a 0.35 g/l AgNO₃ aqueous solution in the presences of 2 g/l HBP-NH₂, showed good antibacterial activities against Gram-negative bacteria (Escherichia coli) and Gram-positive bacteria (Staphylococcus aureus). A very low concentration of nano-silver (as low as 3.0 ug/ml Ag) also gave excellent antibacterial performance.     

Synthesis of hierarchical CuO microspheres: Photocatalytic and antibacterial activities

In this work, hierarchical CuO micropeony was synthesized by an environmentally benign reflux condensation approach without using any surfactant or templates. X-ray diffraction (XRD) analysis revealed the formation of CuO exhibiting monoclinic crystal structure. Fourier transform infrared spectroscopy (FTIR) further confirmed the formation of single phase CuO. Scanning electron microscopy (SEM) analysis showed that the hierarchical CuO architecture is composed of numerous interpenetrating nanosheets that radiated from the center to form floral pattern with a diameter of 1–2 μm. Photoluminescence (PL) spectra of CuO exhibited both UV and visible emissions. The photocatalytic activity of hierarchical CuO microsphere was evaluated by monitoring the photodegradation of methyl orange dye while the antibacterial activity was studied against gram-positive and gram-negative bacteria's. Results demonstrated that CuO hierarchical architecture possesses good photocatalytic as well as antibacterial activity.     

Highly bacterial resistant silver nanoparticles: synthesis and antibacterial activities

In this article, we describe a simple one-pot rapid synthesis route to produce uniform silver nanoparticles by thermal reduction of AgNO₃ using oleylamine as reducing and capping agent. To enhance the dispersal ability of as-synthesized hydrophobic silver nanoparticles in water, while maintaining their unique properties, a facile phase transfer mechanism has been developed using biocompatible block co-polymer pluronic F-127. Formation of silver nanoparticles is confirmed by X-ray diffraction (XRD), transmission electron microscopy (TEM) and UV–vis spectroscopy. Hydrodynamic size and its distribution are obtained from dynamic light scattering (DLS). Hydrodynamic size and size distribution of as-synthesized and phase transferred silver nanoparticles are 8.2 ± 1.5 nm (σ = 18.3%) and 31.1 ± 4.5 nm (σ = 14.5%), respectively. Antimicrobial activities of hydrophilic silver nanoparticles is tested against two Gram positive (Bacillus megaterium and Staphylococcus aureus), and three Gram negative (Escherichia coli, Proteus vulgaris and Shigella sonnei) bacteria. Minimum inhibitory concentration (MIC) values obtained in the present study for the tested microorganisms are found much better than those reported for commercially available antibacterial agents.     

Copper and Graphene activated ZnO nanopowders for enhanced photocatalytic and antibacterial activities

ZnO, ZnO:Cu and ZnO:Cu:Graphene nanopowders were synthesized via a facile wet chemical method. The XRD studies show that the synthesized samples have hexagonal wurtzite structure. It is found that graphene addition induces a decrease in crystallite size. UV–vis absorption spectra of the samples show sharp absorption edges around 380 nm. Photoluminescence studies reveal that the incorporation of copper and graphene in ZnO facilitates the efficient photo generated electron–hole pair separation. It is found that the ZnO:Cu and ZnO:Cu:Graphene nanopowder exhibit improved photocatalytic efficiency for the photodegradation of Methylene Blue (MB) under visible light irradiation. Moreover, improved antibacterial activity of ZnO:Cu:Graphene nanopowder against Escherichia coli and Staphylococcus aureus bacteria is observed.     

Combination of ultrasound-peracetic acid washing and ultrasound-assisted aerosolized ascorbic acid: A novel rinsing-free disinfection method that improves the antibacterial and antioxidant activities in cherry tomato

Traditional ultrasound (US)-assisted disinfection is only effective during washing. Coating is an effective method to control microbial growth after washing; however, cross-contamination can occur during immersion in the coating aqueous solution. Tap water (TW) rinsing is generally used to remove sanitizer residues after US-assisted washing; however, the Food and Drug Administration stated that rinsing is unnecessary when the peracetic acid (PAA) concentration does not exceed 80 ppm. In this study, we proposed a novel US-assisted hurdle technology of 80 ppm PAA combined with low-frequency US (25 kHz) during washing, followed by US-assisted aerosolization processing (nonimmersion coating). Ascorbic acid (AA), a safe and low-cost agent, was selected as the aerosolization solution. Cherry tomatoes were selected as the model, and the proposed method was compared with traditional US-assisted disinfection methods (US-10 ppm free chlorine washing + TW rinsing and US-5 ppm chlorine dioxide washing + TW rinsing) to analyze the disinfection efficacy and quality changes. During storage, US-PAA + 1%AA facilitated additional 0.7–0.9, 0.6–0.8, 0.7–1.0, and 0.5–1.0 log CFU/g reductions in the counts of Escherichia coli O157:H7, Salmonella Typhimurium, aerobic mesophilic counts, and molds and yeasts, respectively, as compared with traditional US-assisted methods. Sensory properties, color index, total soluble solids, titratable acidity, and weight loss were not negatively affected by any of the treatments. Firmness was slightly reduced after all treatments; however, the firmness of the samples was maintained during storage, in contrast with the decreased firmness observed in the control. Phenolic content and antioxidant activity significantly increased after all treatments. Further analysis of two key enzymes (phenylalanine ammonia-lyase and 4-coumarate-CoA ligase) involved in phenolic synthesis showed that their levels significantly increased following all treatments, leading to an increase in phenolic content and antioxidant activity. This result also indicated that US-assisted washing could act as an abiotic elicitor to increase nutritional content. Overall, US-PAA + 1%AA treatment served as an effective method for disinfecting produce during washing and for controlling microbial growth after washing without prolonging the processing time, which is an advantage over traditional US-assisted washing.     

Novel and efficient one-pot five- and six-component reactions for the stereoselective synthesis of highly functionalized enaminones and dithiocarbamates

Efficient methods for stereoselective synthesis of polyfunctional (E)-enaminones and (Z)-dithiocarbamates via one-pot five- and six-component sequential Ugi/Nucleophilic addition reactions are described. High yields and high bond forming efficiency, and simple operations are the advantages of this method.     

Microwave-assisted one-pot multi-component reaction: synthesis of novel and highly functionalized 3-(pyranyl)- and 3-(dihydropyridinyl)indole derivatives

One-pot multi-component reaction of 3-cyanoacetyl indole, aromatic aldehydes and ethyl acetoacetate in the presence of \(\hbox {InCl}_{3}/\hbox {NH}_{4}\) OAc under microwave irradiation for 2–7 min afforded novel and highly functionalized 3-(pyranyl)- and 3-(dihydropyridinyl)indole derivatives, respectively, in good yield.     

Conventional and microwave-assisted synthesis of new indole-tethered benzimidazole-based 1,2,3-triazoles and evaluation of their antimycobacterial,antioxidant and antimicrobial activities

A new series of triheterocycles containing indole–benzimidazole-based 1,2,3-triazole hybrids have been synthesized in good yields via a microwave-assisted click reaction. All the compounds were characterized by IR, \(^{1}\hbox {H}\) NMR, \(^{13}\hbox {C}\) NMR and mass spectroscopy and were evaluated for their in vitro antitubercular activity against the Mycobacterium tuberculosis H37Rv strain. Compounds 4b, 4h and 4i displayed highly potent antitubercular activity with MIC 3.125–6.25 \(\upmu \hbox {g}/\hbox {mL}\). The antioxidant potential was evaluated using 2,2-diphenyl-1-picryl hydrazine and \(\hbox {H}_{2}\hbox {O}_{2}\) radical scavenging activity, and compounds 4e,4f and 4g showed excellent radical scavenging activity with \(\hbox {IC}_{50}\) values in the range of 08.50–10.05 \(\upmu \hbox {g}/\hbox {mL}\). Furthermore, the compounds were evaluated for antimicrobial activity against numerous bacterial and fungal strains, and compounds 4b, 4c and 4h were found to be the most promising potential antimicrobial molecules with MIC 3.125–6.25 \(\upmu \hbox {g}/\hbox {mL}\).     

Optimization of ultrasound-assisted extraction of bioactive compounds from coffee pulp using propylene glycol as a solvent and their antioxidant activities

In the cosmetic and pharmaceutical industries, it has been increasingly popular to use alternative solvents in the extraction of bioactive compounds from plants. Coffee pulp, a by-product of coffee production, contains different phenolic compounds with antioxidant properties. The effects of polyols, amplitude, extraction time, solvent concentration, and liquid–solid ratio on total phenolic content (TPC) using ultrasound-assisted extraction (UAE) were examined by single-factor studies. Three main factors that impact TPC were selected to optimize the extraction conditions for total phenolic content (TPC), total flavonoid content (TFC), total tannin content (TTC), and their antioxidant activities using the Box-Behnken design. Different extraction methods were compared, the bioactive compounds were identified and quantified by liquid chromatography triple quadrupole mass spectrometer (LC-QQQ), and the cytotoxicity and cellular antioxidant activities of the extract were studied. According to the response model, the optimal conditions for the extraction of antioxidants from coffee pulp were as follows: extraction time of 7.65 min, liquid–solid ratio of 22.22 mL/g, and solvent concentration of 46.71 %. Under optimized conditions, the values of TPC, TFC, TTC, 1,1-diphenyl-2-picryl-hydrazil (DPPH) radical scavenging assay, 2,2′-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS) radical scavenging assay, and Ferric reducing antioxidant power assay (FRAP) were 9.29 ± 0.02 mg GAE/g sample, 58.82 ± 1.38 mg QE/g sample, 8.69 ± 0.25 mg TAE/g sample, 7.56 ± 0.27 mg TEAC/g sample, 13.59 ± 0.25 mg TEAC/g sample, and 10.90 ± 0.24 mg FeSO₄/g sample, respectively. Compared with other extraction conditions, UAE with propylene glycol extract (PG-UAE) was significantly higher in TPC, TFC, TTC, DPPH, ABTS, and FRAP response values than UAE with ethanol (EtOH-UAE), maceration with propylene glycol (PG-maceration), and maceration with ethanol (EtOH -maceration) (p < 0.05). Major bioactive compounds detected by LC-QQQ included chlorogenic acid, caffeine, and trigonelline. At higher concentrations starting from 5 mg/ml, PG-UAE extract showed higher cell viability than EtOH-UAE in both cytotoxicity and cellular antioxidant assays. The researcher expects that this new extraction technique developed in this work could produce a higher yield of bioactive compounds with higher biological activity. Therefore, they can be used as active ingredients in cosmetics (anti-aging products) and pharmaceutical applications (food supplements, treatment for oxidative stress-related diseases) with minimal use of chemicals and energy.     

Efficient spectral-Galerkin methods for systems of coupled second-order equations and their applications

We construct in this paper two efficient spectral-Galerkin algorithms for solving systems of n coupled second-order equations. The computational complexity of these algorithms is essentially n times the cost of solving one second-order equation. We present numerical results which illustrate the accuracy and flexibility of these algorithms, as well as several interesting and challenging applications, including in particular a number of high-order nonlinear parabolic type equations.     

Phytochemicals in Capsicum oleoresin from different varieties of hot chilli peppers with their antidiabetic and antioxidant activities due to some phenolic compounds

Due to its wide use in nutritional therapy, a capsicum oleoresin extraction from hot chilli pepper was optimized using ultrasound assisted extraction. Under optimal conditions, a 0.1 g sample in 10 mL of a 20% water in methanol solution was extracted at 50 °C for 20 min to remove phytochemicals consisting of oleoresin, phenolics, carotenoids, flavonoids, capsaicinoids (pungency level), reducing sugars. Antioxidant and antidiabetic activities of the crude extracts from 14 chilli pepper varieties were examined. The antioxidant and antidiabetic activities of some phenolic compounds were also tested individually. The results showed that these chilli pepper samples are a rich source of phytochemicals with antioxidant and antidiabetic activities. High antioxidant activity of the extracts was evaluated using the 2,2-diphenyl-1-picrylhydrazyl, N,N-dimethyl-p-phenylenediamine dihydrochloride, 2,2′-azino-bis(3-ethylbenzothiazolin-6-sulfonic acid) and ferric ion reducing antioxidant power assays. The crude extracts had a lower level of sugars induced by the inhibitory effect of α-amylase activity. Thus, their enzymatic inhibitory effect might have resulted from a synergism among the phytochemicals concerned. Therefore, a diet with this type of food may have beneficial health effects.     

Multicomponent reactions of ammonium thiocyanate,acyl chlorides,alkyl bromides,and enaminones: A facile one-pot synthesis of thiophenes

An efficient synthesis of thiophene derivatives is described via one-pot reaction between ammonium thiocyanate, acyl chlorides, α-halocarbonyls, and enaminones under solvent-free conditions at 65 °C. The mild reaction conditions and high yields of the products exhibit the good synthetic advantage of these methods.     

Sustainable extraction of ligustilide and ferulic acid from Angelicae Sinensis Radix,for antioxidant and anti-inflammatory activities

The 2030 Agenda for Sustainable Development envisions a rational use of energy and resources in all technological processes. However, in the extraction methods of compounds from medicinal plants and herbs, there is an urgent to reduce the use of organic solvents and increase the energy efficiency of these methods. Therefore, a sustainable extraction method (enzyme and ultrasonic co-assisted aqueous two-phase extraction, EUA-ATPE) of simultaneous extraction and separation of ferulic acid and ligustilide from Angelicae Sinensis Radix (ASR) was developed by integrating enzyme-assisted extraction (EAE) with ultrasonic-assisted aqueous two-phase extraction (UAE- ATPE). The effects of different enzymes, extraction temperature, pH, ultrasonic time, liquid-to-materials ratio, etc., were optimized by single-factor experiments and central composite design (CCD). Under the optimum conditions, the highest comprehensive evaluation value (CEV) and extraction yield were obtained by EUA-ATPE. Furthermore, recovery (R), partition coefficient (K), and scanning electron microscopy (SEM) analysis revealed that enzyme and ultrasonic treatment improved mass transfer diffusion and increased the degree of cell disruption. Besides, the EUA-ATPE extracts have shown great antioxidant and anti-inflammatory activity in vitro. Finally, compared to different extraction methods, EUA-ATPE achieved higher extraction efficiency and higher energy efficiency due to the synergistic effect between EAE and UAE-ATPE. Therefore, the EUA-ATPE provides a sustainable method for extracting bioactive compounds from medicinal plants and herbs, contributing to Sustainable Development Goals (SDG), including SDG-6, SDG-7, SDG-9, SDG-12, and SDG-15.     

A discrete KdV equation hierarchy: continuous limit,diverse exact solutions and their asymptotic state analysis

In this paper, a discrete KdV equation that is related to the famous continuous KdV equation is studied. First, an integrable discrete KdV hierarchy is constructed, from which several new discrete KdV equations are obtained. Second, we correspond the first several discrete equations of this hierarchy to the continuous KdV equation through the continuous limit. Third, the generalized (m, 2N − m)-fold Darboux transformation of the discrete KdV equation is established based on its known Lax pair. Finally, the diverse exact solutions including soliton solutions, rational solutions and mixed solutions on non-zero seed background are obtained by applying the resulting Darboux transformation, and their asymptotic states and physical properties such as amplitude, velocity, phase and energy are analyzed. At the same time, some soliton solutions are numerically simulated to show their dynamic behaviors. The properties and results obtained in this paper may be helpful to understand some physical phenomena described by KdV equations.