An overview on synthesis and reactions of coumarin based compounds

Oxygen-containing heterocycles are largely distributed in natural and synthetic compounds. Coumarins are among the most famous heterocycles which possess one oxygen atom in their rings. Coumarins are classified as multifunctional scaffold and are used as anti-oxidant reagents, anti-inflammatory, anti-microbial, anti-fungal, anti-HIV active, analgesic, anti-histaminic, insecticides, dyes, herbicides, sensitizers, perfumes, cosmetics and food additives. Due to their diverse applications in industrial and pharmaceutical fields, many chemists have given significant interest to these compounds. Herein, the review highlights various methods for the synthesis and interactions of coumarin moiety as one of the most efficient categories of heterocycles.

Sequential Four-Component Synthesis And Antitumor Activity Screening of Spiro[chromene-indolo[2,1-b]quinazoline] And Spiro[indolo[2,1-b]Quinazoline-pyrano[3,2-c]chromene]

Chemotherapy is one of the most common types of treatment among cancer patients and by using potent chemicals and agents, tumor promotion was inhibited. Despite the usage of many chemical agents in cancer therapy, cancer is still incurable. It seems that the synthesis of new compounds with high efficiency on cancer cells and low side effects on normal cells will remain a critical challenge among researchers in this area. In the present work, a fast and straightforward process for the transformations involving tryptanthrins, malononitrile, some types of CH-acids such as 1,3-cyclohexanedione, dimedone, and 4-hydroxycumarin resulting in preparing spiro[chromene-indolo[2,1-b]quinazoline] and spiro[indolo[2,1-b]quinazoline-pyrano[3,2-c]chromene] derivatives through sequential Knoevenagel/Michael/intramolecular cyclization sequences was reported. at room temperature. This protocol benefits some notable advantages including short reaction time, mild reaction condition, and simple purification, which make it interesting. Furthermore, it was carried out at room temperature, so it is according to green chemistry procedures. Also, antitumor screening of our new synthetic compounds (4a-i) was evaluated on pancreatic cancer cells (Panc1), breast cancer cells (MDA-MB-231), prostate cancer cells (PC3), and normal human adult dermal fibroblast cells (HDF) by using MTT assay using etoposide as a positive control. We found that 50% growth inhibitory concentration (IC50) values of our synthetic compounds were not lower than etoposide against three cancer cell lines.

Ateleia glazioveana and Ocimum basilicum: plants with potential larvicidal and repellent against Aedes aegypti (Diptera, Culicidae)

The Aedes aegypti is the main vector of the transmission of diseases such as dengue, yellow fever, Chikungunya, and Zika. The agents used for the control of mosquito involve the use of synthetic compounds, which may cause toxicity and contamination environmental. Aiming to test the effectiveness of natural products, the aim of this study was to evaluate the larvicidal and repellent activity of extracts of Ateleia glazioveana Baill. (timbó) and essential oil of Ocimum basilicum L. (manjericão), against A. aegypti. The activities of hydroalcoholic (HEA) and dichloromethane (DEA) extracts from A. glazioveana against A. aegypti larvae were assessed after exposure for 24, 48, and 72 h, using water and Bacillus thuringiensis israelensis as negative and positive controls, respectively. For repellent evaluation, we investigated the sting attempts of A. aegypti in response to the application of HEA- and DEA-based body creams (5%), as well as an alcoholic spray based on the essential oil from O. basilicum. The repellency of these preparations was compared with negative (vehicle) and positive (DEET) controls. Although HEA showed no apparent larvicidal activity, DEA at concentrations of 150 to 500 mg/ml showed high larvicidal potential after 24 h, compared to the negative control group (p < 0.001). Moreover, the DEA-based cream and the alcoholic spray of O. basilicum based essential oil showed higher repellency compared with the vehicle (84.5% and 70.5%, respectively). Accordingly, it is possible to infer that extracts and preparations of A. glazioveana and O. basilicum exhibit larvicidal and repellent activity against A. aegypti.

Кореферентные структуры, используемые для представления экономических субъектов в медийном дискурсе

The subject of study in the article is the discourse specifics of representation of economic entities in German newspaper and magazine texts of the last two decades. The purpose of the analysis is to elucidate the factors that stimulate univerbation in connection with the generation and textual integration of co-referential structures different in genesis, structural properties, semantic characteristics and stylistic potential. The study, conducted on the basis of a functional-communicative approach to language, relies on methods and results of studies on text linguistics considering text as a whole structural-semantic unit. Conclusions. 1) Mentioning of a company name is accompanied by integration of the univerb indicating the relevant industry into the text. Along with a two-member chain of co-referential nominations, a three-member chain is also possible (the location of a company is mentioned). 2) Co-referential pairs of the type “company name ‒ collective designation of employees according to headquarters location” (Siemens ‒ Münchener) are characteristic, which demonstrates the lability of univerb toponym semantics. 3) The integration of a proper name into the text requires the usage of characterizing common nouns in order to prepare the reader for the perception of unique names, which is a factor motivating univerbation. 4) Synthetic compounds of the nomina agentis type (Autobauer, Stromversorger) are widely used to describe the kind of activity of an enterprise. In such cases a lexeme with the expected semantics is eliminated (Unternehmen ‘company’, Konzern ‘concern’ etc.). The reduction of the base lexeme of a compound as well as representation of the verb lexeme in the form of nomen agentis has an impact on the semantics and stylistics of the univerb. The results of the study can be used both in research activities on problems of word-formation, semantics and in the training of business translators.

A Mini-Review: Recent Advances in Coumarin-Metal Complexes With Biological Properties

The coumarin nucleus is a recurring motif in both natural and synthetic compounds that exhibit a broad spectrum of biological properties including anticoagulant, anti-inflammatory, antioxidant, antiviral, antimicrobial and anticancer agents as well as enzyme inhibitors. On the other hand, it has been reported that the incorporation of a metal ion into coumarin derivatives can increase the activity of such complexes compared to coumarin-based ligands. Accordingly, some of them have been found to display promising antioxidant, antitumor or antibacterial activities. This mini-review briefly summarizes the recent development of coumarin-metal complexes with proven biological properties. The attention is also paid to agents for which practical applications in the detection of biologically important species may be found.

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Design, Synthesis, Reactions and Antibacterial Properties of 2-hydrazinyl-3-methyl-6-nitroquinoxaline Derivatives

Aims: This aims of this study was to synthesis new quinoxaline-based heterocycles and study its antibacterial properties. Objective: This study was designed to synthesis some 3-methyl-6-nitroquinoxaline-2-one with hydrazine moiety, characterize the synthesized compounds, and study their antibacterial properties on some bacterial strains. Materials and Methods: Six 3-methylquinoxaline-2-hydrazone derivatives were synthesized by reacting 2-hydrazinyl-3-methyl-6-nitroquinoxaline with various substituted acetophenones. The hydrazones were screened for their potential antibacterial properties. Results: All the test compounds were found to possessed promising antibacterial properties against a panel of bacterial strains screened for this study. The MIC values exhibited by these compounds ranged between 0.0313 and 0.250 mg/mL. The lowest MBC of the compounds against the test organism was 0.0625 mg/mL while the highest MBC was 0.250 mg/mL. Discussion and Conclusion: The study concluded that all the compounds exhibited appreciable bactericidal effects against all the bacterial strains, which is an indication that such synthetic compounds possessed broad spectrum activities and such compounds could be useful in formulation of antibacterial compounds which could be used to mitigates infections caused by pathogens that are now developing resistance against the available antibiotics.

Advanced Bioinformatics Tools in the Pharmacokinetic Profiles of Natural and Synthetic Compounds with Anti-Diabetic Activity

Diabetes represents a major health problem, involving a severe imbalance of blood sugar levels, which can disturb the nerves, eyes, kidneys, and other organs. Diabes management involves several synthetic drugs focused on improving insulin sensitivity, increasing insulin production, and decreasing blood glucose levels, but with unclear molecular mechanisms and severe side effects. Natural chemicals extracted from several plants such as Gymnema sylvestre, Momordica charantia or Ophiopogon planiscapus Niger have aroused great interest for their anti-diabetes activity, but also their hypolipidemic and anti-obesity activity. Here, we focused on the anti-diabetic activity of a few natural and synthetic compounds, in correlation with their pharmacokinetic/pharmacodynamic profiles, especially with their blood-brain barrier (BBB) permeability. We reviewed studies that used bioinformatics methods such as predicted BBB, molecular docking, molecular dynamics and quantitative structure-activity relationship (QSAR) to elucidate the proper action mechanisms of antidiabetic compounds. Currently, it is evident that BBB damage plays a significant role in diabetes disorders, but the molecular mechanisms are not clear. Here, we presented the efficacy of natural (gymnemic acids, quercetin, resveratrol) and synthetic (TAK-242, propofol, or APX3330) compounds in reducing diabetes symptoms and improving BBB dysfunctions. Bioinformatics tools can be helpful in the quest for chemical compounds with effective anti-diabetic activity that can enhance the druggability of molecular targets and provide a deeper understanding of diabetes mechanisms.

Exogenous Application of Biostimulants and Synthetic Growth Promoters Improved the Productivity and Grain Quality of Quinoa Linked with Enhanced Photosynthetic Pigments and Metabolomics

Modern agriculture is mainly concerned with maximum resource use efficiency linked with greater productivity to feed the growing global population. The exogenous application of biostimulants is considered a sustainable approach to improve the growth and productivity of field crops. The present study was carried out to explore the comparative impact of biostimulants and synthetic compounds on quinoa crop (cultivar UAF-Q7), as it has gained significant popularity among agricultural scientists and farmers throughout the world, due to its high nutritional profile. A two-year field experiment was carried out at the Research Area of Directorate of Farms, University of Agriculture, Faisalabad, Pakistan. Application of moringa leaf extract (MLE) produced the maximum total chlorophyll (5.11 mg g−1) and carotenoids (1.2 mg g−1), compared with the control. Antioxidants’ activities and gas exchange attributes were also recorded as the highest following MLE application. Mineral elements in root and in shoot were found highest in response to MLE application. Similarly, application of MLE significantly improved the growth and yield attributes of quinoa. Mineral elements of grain (Mg, Zn and Fe) were also significantly enhanced. MLE was found to be more responsive in improving the growth and quality compared with synthetic compounds.

Plant-Derived Substances with Antibacterial, Antioxidant, and Flavoring Potential to Formulate Oral Health Care Products

Bacterial diseases and reactive oxygen species can cause dental caries and oral cancer. Therefore, the present review analyzes and discusses the antibacterial and antioxidant properties of synthetic and plant-derived substances and their current and future patents to formulate dental products. The reviewed evidence indicates that chlorhexidine, fluorides, and hydrogen peroxide have adverse effects on the sensory acceptability of oral care products. As an alternative, plant-derived substances have antimicrobial and antioxidant properties that can be used in their formulation. Also, adding plant metabolites favors the sensory acceptability of dental products compared with synthetic compounds. Therefore, plant-derived substances have antibacterial, antioxidant, and flavoring activity with the potential to be used in the formulation of toothpaste, mouth rinses, dentures cleansers-fixatives, and saliva substitutes.