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A one-pot procedure for the synthesis of azolopyrimidine derivatives by a three-component reaction of β-ketosulfone, aldehyde, and 2-aminoben-zimidazole over synthetic magadiite clay (SMC-H) under ball milling in the absence of any solvent and additive has been developed. The catalyst was re-used for consequent reactions. The novel manufactured compounds were verified for HePG2 cell development inhibition. A pronounced inhibitory effect on the growth of HePG2 cell line was recorded. This protocol offers a broad scope for an access to a variety of diversely substituted azolopyrimidines of high inhibition activity against HePG2 cell line. The use of non-hazardous organic solvent, ball milling, cost efficiency, recyclability of the catalyst up to six runs without appreciable loss of activity, and high yields of products make this procedure greener. [ABSTRACT FROM AUTHOR]

In this study, an efficient regioselective synthesis of a novel pyrazole derivative containing a coumarin moiety (PC) was achieved. Unambiguous structural assignment of the obtained regioisomers was performed using two-dimensional heteronuclear multiple bond correlation (2D HMBC) NMR spectroscopy as a valuable tool. A Co2+ ion-selective electrochemical sensor was fabricated by depositing the synthesized pyrazole derivative on a glassy carbon electrode (GCE) and the electrochemical method was investigated in detail in phosphate buffer medium. The proposed Co2+ ion sensor exhibited a linear relationship for current vs. Co2+ ion concentration in the concentration range of 0.1 nM to 0.01 mM, denoted as the linear dynamic range, demonstrating an appreciable sensitivity of 19.9146 μA μM−1 cm−2. From a signal-to-noise ratio of 3, the estimated limits of detection and quantification were 94.04 ± 4.70 pM and 313.47 pM, respectively. The Co2+ ion sensor comprising PC deposited on a GCE showed good electrochemical sensing performance, with precise reproducibility, a short response time, and good reliability. The proposed Co2+ ion sensor provides an efficient route to detect Co2+ ions for environmental remediation using pyrazole derivatives. [ABSTRACT FROM AUTHOR]

A sustainable, green one-pot process for the synthesis of dihydropyrimidinones (DHPMs) derivatives by a three-component reaction of β-ketoester derivatives, aldehyde and urea or thiourea over the alkali-treated H-ZSM-5 zeolite under ball-milling was developed. Isolation of the product with ethyl acetate shadowed by vanishing of solvent was applied. The hierachical zeolite catalyst (MFI27_6) showed high yield (86%-96%) of DHPMs in a very short time (10-30 min). The recyclability of the catalyst for the subsequent reactions was examined in four subsequent runs. The catalyst was shown to be robust without a detectable reduction in catalytic activity, and high yields of products showed the efficient protocol of the Biginelli reactions. [ABSTRACT FROM AUTHOR]

Background: Most of the known approaches to the synthesis of CF3-containing organic compounds suffer from serious drawbacks. For example the starting materials required for these methods are rather difficult to obtain, or they are fairly toxic and inconvenient to work with and methods for direct fluorination and trifluoromethylation do not always allow the introduction of the CF3-group at the required position of a molecule. Results: An efficient and attractive regioselective synthesis of a series of novel pyrazoles containing the trifluromethyl moiety was achieved using Cu(OTf)2/Et3N as an efficient catalytic system under ultrasonic irradiation. Conclusions: Cu(OTf)2/Et3N catalyst showed a great advantage over all the investigated catalysts, and the ultrasonic irradiation method offered high yields of pyrazoles in short reaction time compared with classical conditions. gHMBC spectra of the product were used to rationalize the observed regioselectivity. [ABSTRACT FROM AUTHOR]

Abstract: SiO2–Al2O3 support material was prepared by sol–gel method, followed by calcination at 500, 1000 and 1500°C. The supported nickel catalyst containing 5wt% was obtained by impregnating a known mass of the calcined support material with nickel sulfate solution followed by drying and reduction with hydrazine hydrate at 80–100°C. The prepared catalysts were fully characterized by XRD and SEM, EDX and ESR. The hydrogenation of p-nitrophenol into p-aminophenol was performed using hydrazine hydrate as hydrogen donor. The product of the reaction was examined using IR, and NMR. The results showed that the degree of crystallinity of the support affects the catalytic activity of nano-sized Ni catalyst. It was observed that as the degree of crystallinity of the support material increases the catalytic activity increases. On the other hand, intermolecular interaction between nano-nickel clusters disappears completely in samples whose support was calcined at 1500°C. [Copyright &y& Elsevier]

The emergence of Candida auris poses a significant global health threat due to its high mortality rates and multidrug resistance. The development of new antifungal drugs is essential to effectively combat this pathogen. Antimicrobial peptides, such as Dermaseptin, have demonstrated potent anti- Candida activity. This study aimed to investigate the antifungal activity of Dermaseptin against C. auris isolates and its ability to induce oxidative stress and apoptosis. The results revealed the robust anti- Candida activity of Dermaseptin, with a minimum inhibitory concentration (MIC) of 15.62 μg mL -1 and a minimum fungicidal concentration (MFC) of 31.25 μg mL -1 . Spectrophotometric analysis demonstrated that Dermaseptin induced significant oxidative stress, as evidenced by the notable differences in the activity of primary antioxidant enzymes and lipid peroxidation (LPO) levels between the treated and untreated control groups. Moreover, Dermaseptin influenced the gene expression of antioxidant enzymes, as confirmed by reverse transcription quantitative polymerase chain reaction (RT-qPCR). Additionally, Dermaseptin induced apoptosis in C. auris in a dose-dependent manner. This study highlights the potential of Dermaseptin to inhibit and potentially eradicate C. auris by increasing oxidative stress levels. The low MICs and fungicidal properties of Dermaseptin against C. auris isolates suggest its potential as a candidate for the development of a novel antifungal agent., Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (This journal is © The Royal Society of Chemistry.)