Chemistry Proceedings, Volume 3, Issue 1

(2E)-3-(3,4-Dichlorophenyl)-N-arylprop-2-enanilides were designed as potential bioactive agents. Six compounds were mono- and di-chlorinated also on the anilide ring. Since the biological activities of molecules are influenced by lipophilicity, the h...

Polyphenols are attracting increasing attention in the discovery of useful agents for the treatment of neurodegenerative diseases. Thelesperma megapotamicum (Spreng.) Kuntze belongs to the family Asteraceae, which is known to have a high antioxidant...

Limonium brasiliense (Boiss.) Kuntze (Plumbaginaceae) is a medicinal plant that is popularly used in the folk medicine. In this study, we examined xanthine oxidase (XO) inhibitory activity of the aqueous fraction of Limonium brasiliense extract and i...

Organophosphorus compounds play an important role in the medicinal- or agricultural industry, and in the human body as well. Over the last years, heterocyclic phosphonates have received growing interest due to their potential biological activity. An...

2,4,6-Trichloro-1,3,5-triazine (TCT) offers the unique ability to undergo sequential nucleophilic substitution reactions using regular nucleophiles (first Cl replacement at 0 °C, second at RT, and third at >90 °C), making s-triazine a privileged s...

An efficient and sustainable copper-catalyzed protocol has been developed for the preparation of amidines via nucleophilic addition of amines into nitriles. The reaction proceeded smoothly at 100 °C in the presence of CuCl, Cs₂CO₃, and 2,2^/-bipyridin...

Iminosugars are sugar mimetics present in plants and microorganisms that were first reported in the 1960s. [...]

It has been found that usnic acid carbonyl groups can be hydrogenated by the action of H₂/Pd(C). Thus, two new dibenzofuran derivatives were synthesized.

The presence of tetrahydropyrans and other sized oxacycles in natural products with interesting pharmacological properties has prompted researchers to try to develop new strategies for their selective synthesis. Moreover, these methodologies enable t...

New heterocyclic derivatives of usnic acid have been obtained by the reaction of bromousnic acid with CS₂-based nucleophiles. A series of compounds with dithiolane, 1,3,4-thiadiazine, and thiophene fragments was synthesized.

The copper-catalyzed regioselective intermolecular hydroamination of terminal alkynes with amines was accomplished. The reaction was catalyzed by copper nanoparticles supported on montmorillonite K10 (CuNPs/MK10) and afforded the desired imines in go...

The sensing behavior of a calix[4]arene-oxacyclophane-carbazole conjugate (1) towards Cu(I) ions was investigated. Contrary to the noteworthy sensitivity and selectivity previously found for Cu(II), the affinity of 1 for Cu(I) cations is much lower....

Reactions of dinitrobenzoannulated heterocycles (furazan, thiadiazole, selenadiazole, pyridine) with anionic C-nucleophiles (mono- and diketones, nitroalkanes and related compounds) provided stable anionic adducts in high yields. Consecutive oxidatio...

A novel synthetic strategy to obtain acylhydrazone-oxazole hybrids in three-step reactions in moderate to good yields is reported. The key step reaction consists in a Van Leusen reaction using a bifunctional component of both an aldehyde and a functi...

: A copper-based metal-organic framework with 1,3,5-tricarboxylic acid linkers was prepared through a facile hydrothermal method. This MOF has not been used in organic reactions widely. Cu.BTC was employed as an affordable, competent heterogeneous ca...

3-(Biphenyl)acrylates are prepared in good yield by one-pot Suzuki cross-coupling (Wittig olefination reactions). The central building blocks are 4-formyl- and 3-formylphenylboronic acids and the stabilized (carbomethoxymethylene)triphenylphosphorane...

The synthesis and characterization of a new fluorogenic substrate for granzyme B (GzmB) is reported. The substrate design was based on the fluorescence resonance energy transfer (FRET) principle using 5-(2′-aminoethyl)aminonaphthalene sulfonic acid (...

Palladium has wide application in different contexts and, as a consequence, high levels of palladium in the environment have been reported, representing a risk to human health. Considering the interest to develop more selective and sensitive chemose...

Ten natural and semi-synthetic compounds (gallic acid and alkyl gallates) were investigated by in silico methods in order to evaluate their potential inhibitory activity against SAR-CoV-2 using the X-ray structure of SARS-CoV-2 main protease bound to...

Drug repositioning involves the investigation of existing drugs for new therapeutic purposes, such as type 2 diabetes. This disease affects the health and quality of life for individuals around the world. Sitagliptin, a highly selective dipeptidyl pe...

: Aphis craccivora is an aphid which damages many species of plants and is also a vector for numerous plant viruses. Since neonicotinoids are a well-known class of effective insecticides with less toxicity against mammals and other vertebrates, a sma...

Fucooligosaccharides comprise the primary group of human milk oligosaccharides. Due to their beneficial properties, a series of synthetic methods have been proposed to obtain them. Enzymatic methods show great promise, and α-l-fucosidase from Thermot...

The relationship between properties of aromatic polyamides and the structure and pKa of substituted diamine monomers allows for modeling and designing the synthesis of polymers with special properties for different uses (dialysis membranes, ion excha...

New triethylammonium 6-amino-4-aryl-3-carbamoyl-5-cyano-1,4-dihydropyridine-2-thiolates were prepared in good yields by the ternary condensation of malononitrile, aldehydes and monothiomalonamide in the presence of Et₃N. The thiolates underwent S-alk...

Benzofuroxane reacts under Beirut reaction conditions with active methylene nitriles to give new 2-aminoquinoxaline-1,4-dioxides. The treatment of known 2-amino-3-cyanoquinoxaline-1,4-dioxide with chloroacetyl chloride afforded corresponding chloroac...

A new approach for the rapid multi-functionalization of BODIPY dyes towards biophotonics is reported. It is based on novel N-BODIPYs, through reactive intermediates with alkynyl groups to be further derivatized by click chemistry. This approach has b...

An optically active bicyclo[2.2.0]heptane fragment was introduced in the molecule of new 1′-homonucleosides on a 2- 6-chloro-amino-purine scaffold to obtain 6-substituted carbocyclicnucleozide analogs as antiviral compounds. The synthesis was realize...

In the last years, interfacial engineering has played a critical role in promoting the performance of optoelectronic devices as organic solar cells (OSC) and organic light-emitting diodes (OLEDs) since interfacial layers help to form an ohmic contact...

Organophosphorus (OP) chemicals were broadly used as insecticides and in the treatment of human diseases such as malaria mosquitoes, parasitosis, myasthenia, and glaucoma. The OP toxicity is well known. They can cause environmental and health proble...

The high concentration of pesticide residues existing in vegetation, crops, and various edible products and the prolonged exposure to them can harm human life and contribute to the disappearance of honey bees, and several avian and animal species. Th...

Upon treatment with chloroacetyl chloride, 3-aminothieno[2,3-b]pyridines gave the corresponding chloroacetamides. The latter readily react with sodium thiosulphate to afford water soluble S-alkylthiosulphates with pharmacophoric heterocyclic units.

5-Amino-3-(cyanomethyl)-1H-pyrazole-4-carbonitrile, prepared by reaction of malononitrile dimer with hydrazine, smoothly reacts with chloroacetyl chloride to form 2-chloro-N-(4-cyano-3-(cyanomethyl)-1H-pyrazol-5-yl)acetamide in good yield. The latter...

Flavonoids, widely distributed in fruits, vegetables, and medicinal herbs, are compounds with multiple biological benefits to human health from anti-inflammatory, antioxidant, anticancer, antibacterial to antiviral activity. Coronavirus disease 2019...

The genus Coccoloba (Polygonaceae) comprises approximately 150 species of flowering plants. It is native to the tropical and subtropical regions of America, in South America, the Caribbean and Central America. A wide variety of biological activities...

In this work, viscosity, density and electrical conductivity of the ionic liquid, Ethylimidazolium Nitrate pure and doped with lithium nitrate salt were determined in order to check the properties’ improvement of the ionic liquid with the salt additi...

Nano-sized spinel ferrites are highly regarded owing to their special optical, electrical, and magnetic properties. Cobalt ferrite (CoFe₂O₄) is a nominee of particular interest due to its high saturation magnetization, high coercivity, strong anisotr...

Leishmaniasis is a largely neglected infection caused by Leishmania spp. parasites. The first-line treatment, antimoniate meglumine, has a large number of adverse effects, high cost and is prone to resistance development, hence the necessity of new a...

The cycloaddition strategy was employed in order to obtain a 7-oxanorbornene framework substituted with a guanidine moiety or its precursor functional groups: protected amine or thiourea. In order to optimize the conditions for the cycloaddition, sev...

In this work, the synthesis of thiohydantoins from l-amino acids and isothiocyanates was studied, using a high purity method based on the Edman cycle. This process, expected to occur through the Michael addition to a series of 1,4-naphthoquinone deri...

The goal of the present work was to evaluate the chemical reactivity of amino acids with polar uncharged side chains (serine, threonine, asparagine and glutamine) using density functional theory (DFT) and thermodynamics modeling by calculating a ser...

A series of six novel amide-xanthate products containing several fluorine atoms were prepared in moderate to good yields (40–92%) via an isocyanide-based multicomponent reaction (IMCR) of 5-CR by Ugi-4CR followed by an S_N2 sequence in a one-pot manne...

Ultra-fast one-put microwave assisted strategy was introduced for the synthesis of hetero-structured CuCo₂S₄/CuCo₂O₄ nanoparticles into a domestic microwave oven with the power of 900 W for 20 min. Thiourea as an organic agent was used as a sulfur so...

A series of triphenylamine-imidazo[1,2-a]pyridine were synthesized in moderate yields (57–67%) by Groebke–Blackburn–Bienaymé reaction (GBBR) under catalyst and solvent green conditions. The molecules synthesized containing triphenylamine and imidazo[...

Eugenol is a major constituent of clove essential oil with interesting biological activity, namely antimicrobial and antioxidant. Structural changes of eugenol are a useful strategy in order to improve biological activity and at the same time obtain...

Benzophenoxazine fluorophores, including derivatives of Nile Blue, one of the best known in this family of compounds, have been used as histological stains due to their optical properties in the NIR region and stability. Given their potential, the sy...

Advances in different technological and scientific fields have led to the development of tools that allow the design of drugs in a rational way, using defined therapeutic targets, and through simulations that offer a molecular view of the ligand–rece...

In present work we report our studies of the interaction of 1-phenyl-1H-pyrrole-2,5-dione derivatives (N-arylmaleimides) and 3-bromodihydrofuran-2(3H)-one (α-bromo-γ-butyrolactone) as possible [C₂]²⁺ synthons with 1,2,4-triazole-3(5)-thiole targeting...

Compounds with hindered phenolic moiety are known to be effective inhibitors of oxidative processes in different materials; moreover, a number of phenols show a wide spectrum of biological activity. At the same time, five-membered heterocycles exhibi...

As the most abundant protein with a variety of physiological functions, human serum albumin (HSA) has been used extensively for the delivery and improvement of therapeutic molecules. Thiolactone chemistry provides a powerful tool to prepare albumin-b...

Herein, an eco-friendly palladium-catalyzed tandem reaction for the one-pot synthesis of carbazoles under microwave irradiation is reported. This approach involves an amination and a direct arylation from available and inexpensive anilines and 1,2-di...