Synthesis and characterization of some 1, 5-benzodiazepine derivatives from Chalcones and their use as scavengers for some heavy metals in Environmental Systems.

Chalcones (A1-A4) compounds were prepared by reacting an aldehyde (Cinnamaldehyde or terphthaldehyde) with a ketone (4-aminoacetophenone or acetylacetone) in the presence of 30% NaOH as a catalyst and ethanol as a solvent. Derivatives of 1,5-benzodiazepine (A5-A12) were prepared by reacting these prepared chalcones with orthophenylene diamine or 4-methylorthophenylene diamine in a basic medium of sodium hydroxide 10% using the microwave method. Some prepared compounds were used as scavengers of some heavy metals (iron and lead) from heavy water in ecosystems, as the results indicated the ability of these compounds to reduce or withdraw these elements from heavy water. The stability of these compounds was also tested against laser rays, as they showed resistance and stability towards laser rays.

New coating formulation based on synthesized benzodiazepine derivatives as double function additives for industrial application

Purpose The purpose of this study is to develop a new protective coating formulation for industrial use, using benzodiazepine derivatives as double function additives. Design/methodology/approach Benzodiazepine’s derivatives of types (3–5) were prepared and confirmed by infrared, Mass, 1H-Proton nuclear magnetic resonance (NMR) and 13C NMR spectra. The synthesized compound was physically incorporated in the alkyd paint formulation by pebble mill grinding until all particulates are smaller than 20 ums. The prepared coatings were applied by air spray on steel panels. The physical, mechanical characteristics, corrosion resistance and antimicrobial test of the prepared coatings were studied to evaluate the prepared compounds drawbacks. Findings The results of the mechanical and physical properties of the paint formulation revealed that the paint formulation incorporating benzodiazepines derivatives 3–5 performed best and improved corrosion-resistance and antibacterial activity tests. Research limitations/implications In alkyd paint, heterocyclic compounds are the most used antibacterial additives. Other functionalities of these compounds, such as corrosion inhibitors, might be studied to see if they are suited for these applications. Practical implications Because of the activity of various benzodiazepine derivatives, which may be attributable to the presence of some function groups such as sulfonamide aromatic amino NH2 group, and elements such as Sulphur, Nitrogen, Chlorine, in its chemical structure. As a result, paint compositions including these compounds as additives can be used as dual-purpose paint and for a variety of industrial applications. Originality/value The research demonstrates how a low-cost paint composition based on synthesized benzodiazepine derivatives 3–5 may be used as a dual-function paint for industrial use.

Screening of anxiolytic properties and analysis of structure-activity relationship of new derivatives of 6-(4-methoxy)-7H-[1,2,4]triazolo[3,4-a][2,3]benzodiazepine under the code RD

Introduction: Searching for new compounds with anti-anxiety activity resulting from the combination of privileged scaffolds is a promising direction in medicinal chemistry and in the development of new drugs. Anxiolytic potential and cytotoxic properties of previously synthesized molecules, containing fragments of 2,3-benzodiazepine and 1,2,4-triazole – 6-(4-methoxyphenyl)-7H-[1,2,4]triazolo[3,4-A][2,3]benzodiazepines under the generic code RD were studied. Materials and methods: Screening for anxiolytic activity was performed on elevated plus maze (EPM) and open field (OF) test models. Structural and functional analysis of the anti-anxiety activity of the studied substances was carried out. A degree of muscle relaxant effect of the substances was assessed in the tests Grid, Wire, and Rotarod. A cytotoxicity study of RD compounds was carried out using an MTT assay on human hepatocellular carcinoma cells HepG2. Results and discussion: For a number of novel triazolo[3,4-a][2,3]benzodiazepine derivatives, a prominent anxiolytic activity was manifested in terms of EPM test. The results of OF test were consistent with the obtained data and confirmed the presence of the sought activity in the leading compounds. There was no significant effect on muscle tone for the compounds under study. It was observed that RD compounds possessed no cytotoxic properties and were safe for further studies in vivo. Conclusion: Among the new derivatives of 6-(4-methoxyphenyl)-7H-[1,2,4]triazolo[3,4-a][2,3]benzodiazepine under the code RD, substances (RD-4, 12, 13) with a high anxiolytic activity comparable to diazepam and tofisopam were found. The most promising compound is RD-4 due to its pronounced anxiolytic and low cytotoxic properties.

Trends in the Use of Anxiolytics in Castile and Leon, Spain, between 2015–2020: Evaluating the Impact of COVID-19

Anxiolytics (N05B) are one of the most widely used pharmacological groups. This study aimed to analyze the progression of the consumption of anxiolytics (ATC classification: N05B) dispensed in pharmacies in Castile and Leon, Spain, from 2015 to 2020, with a special focus on the possible impact of COVID-19 on the use of these drugs. A quantitative-qualitative analysis of usage was carried out using the total number of packs and the packs per 1000 inhabitants. Overall, the use of anxiolytics grew by 14.41% during 2015–2020. The most commonly used drugs were the short-acting benzodiazepine derivatives lorazepam (whose use increased by 15.18%) and alprazolam (whose use increased by 21.40%), and the dispensing of the long-acting derivative diazepam increased the most, by 31.83%. Anxiolytics consumption increased significantly in 2020 and peaked in March. The pattern of use remained the same in 2020. The consumption of anxiolytics has continued to increase in Castile and Leon over the last six years. The COVID-19 pandemic situation affected the dispensing of these drugs, causing a sharp increase in prescriptions, especially during March, when the confinement of the population was initiated.