Abstract: Breeding of small cattle is affordable for small farms and does not require signif-icant financial investments, however, forage is often characterized by an insufficient content of minerals and vitamins. The paper analyzes patent developments of mineral and vitamin complexes (MVCs) intended for dry sheep and lambs, as well as a review of scientific data justifying the use of their components. Based on a search in the World Intellectual Property Organization (WIPO) database for the keywords “vitamins for sheep” and “minerals for sheep”, 23 patents focused on dry sheep and lambs were se-lected from 120 patents on feed additives for sheep. Their component composition is analyzed, which is conditionally divided into four groups: minerals, vitamins, func-tional and feed additives. It is shown that modern MVCs are developed taking into account the requirements of environmental safety and the physiological needs of ani-mals. It is concluded that minerals and vitamins should be considered as elements of a scientifically based vitamin and mineral system, the effectiveness of which during pregnancy is determined by the initial level of provision, the physiological status of animals and the characteristics of mineral metabolism.

Abstract:

2-Aryl-2-(3-indolyl)acetohydroxamic acids have emerged as promising antitumor agents; however, their poor pharmacokinetic profile remains a significant drawback. To address this limitation, we have synthesized homologs of such an acids—specifically 2-aryl-2-(3-indolyl)propionic acids—along with several other derivatives. The cytotoxicity of these compounds against glioblastoma cell lines was evaluated and compared to that of the parent acetohydroxamic acid derivatives.

Abstract: The search of new antibacterial agents is an important task due to the emergence of resistance to widely used drugs. The bromine, chlorine and nitro-substituted in phenyl ring azomethines with long alkyl chains (C12, C14, C16 and C18) were synthesized and characterized by several experimental methods (NMR and IR spectroscopy, elemental analysis). Antibacterial activity was tested on several cultures and the synthesized compounds show the activity at the level of some commercial antiseptics. Lipophilicity (which is important descriptor for biological properties prediction) of the experimentally synthesized and isomeric molecules was determined by three different approaches: quantum chemistry, machine learning (GraphormerLogP model) and atom contribution model (RDKit library). Quantum-chemical method can take into account any spatial arrangements and can be considered the most accurate of the used approaches, but a lot of computational time it is necessary for it. Atom contribution model is the fastest of the used methods but gives underestimated results and different isomers have exactly the same values in contrast to the quantum chemistry results. Machine learning-based methods (GraphormerLogP) demonstrate acceptable accuracy, sensitivity to isomerism, and orders of magnitude higher throughput, making them an optimal tool for high-throughput screening.

Abstract: Amino acid derivatives, such as β-keto esters and pyrrolones, were used as nucleophiles in organocatalyzed Michael additions to nitroalkene acceptors, while fatty acid derivatives acted as both nucleophiles (β-keto esters) and electrophile (nitroalkene acceptor). Bifunctional noncovalent organocatalysts were employed as asymmetric organocatalysts. Twenty compounds – including fatty acid and amino acid derivatives, as well as fatty acid–amino acid conjugates – were prepared with enantioselectivities of up to 98% ee. All novel products were fully characterized. This research demonstrates the ease of assembling readily available fatty acid and amino acid building blocks under ambient conditions.

Abstract: Nucleophilic ring-opening of bis(oxiranes), containing several reactive centers, can be used to elaborate straightforward atom-economy and stereoselective approaches to polyfunctionalized compounds. In the present work ring-opening of cis- and trans-diastereomers of a spirocyclic bis(oxirane), containing a cyclooctane core (namely, 1,8-dioxadispiro[2.3.2.3]dodecane), upon the treatment with various amines was studied. Trans-isomer afforded aminoalcohols with 9-oxabicyclo[3.3.1]nonane moiety, formed via domino-process, including opening of an oxirane ring followed by intramolecular cyclization. Ring-opening of cis-isomer gave aminosubstituted cis-cyclooctane-1,5-diols, derived from independent reaction of two oxirane moieties. Activation of oxirane rings by the addition of LiClO4, acting as a Lewis acid, allowed involving a number of primary and secondary aliphatic amines as well as aniline derivatives into the reaction. Scope and limitations of the reaction were studied and a series of aminoalcohols with 9-oxabicyclo[3.3.1]nonane core and symmetric diaminodiols with cyclooctane core were obtained.

Abstract:

A symmetrical rubrene derivative, 5,6-bis(4-(methoxycarbonyl)phenyl)-11,12-diphenyltetracene, was synthesized via the thermal dimerization of 1,1-diphenyl-3-[4-(methoxycarbonyl)phenyl]-3-chloroallene. The reaction proceeded with low selectivity, affording the target tetracene and the bis(alkylidene)cyclobutene by-product in nearly equal yields 25% each. The optical characteristics of this rubrene derivative were investigated, revealing bright orange fluorescence in a CHCl₃ solution (λ_em=565 nm, Φ_F=0.81, τ=11.41 ns), which is strongly quenched in the solid state (Φ_F=0.01) due to aggregation.

Abstract: Currently, prostate specific membrane antigen ligands are one of the most widely used platforms for creating compounds targeting prostate cancer tumor cells. In this mini-review, we have collected and systematized existing approaches to the synthesis of PSMA ligands based on DCL urea, as the most widely used vector platform. The main approaches to each stage of the synthesis of PSMA inhibitors of various structures are considered in detail, and existing synthetic techniques are collected and analyzed.

Abstract: A new series of promising and easily accessible antiproliferative agents based on cy-cloruthenated imines of benzene and thiophene carbaldehydes has been developed and fully characterized using UV-Vis spectroscopy, X-ray diffraction, NMR, HRMS, and cyclic voltammetry. The biological activity of these compounds was tested against A2780, cis-platin-resistant A2780, and HEK293 cell lines, and they exhibited nanomolar IC50 values. They also showed a selectivity index of up to 2.5, indicating their potential as promising antiproliferative compounds.

Abstract: The Kabachnik–Fields (KF) reaction is a versatile three-component condensation of amines, carbonyl compounds, and P–H reagents, enabling efficient synthesis of α-aminophosphonates—key bioactive and functional molecules. This review critically examines the literature of the last 25 years, with the exception of selected mechanistic studies, highlighting mechanistic insights. Advances in catalyst-free methodologies, sustainable synthetic approaches, Lewis and Brønsted acid catalysis are discussed, alongside developments in enantioselective KF reactions in the presence chiral metal complexes or organocatalysts.

Abstract: Terpyridines are well-known ligands in coordination chemistry due to their conforma-tional flexibility and strong metal-binding properties; therefore, they serve as attractive platforms for the design and synthesis of new functional derivatives. This study focused on the synthesis and comprehensive investigation of a new class of bis-oxazolo[5,4-b]pyridine derivatives, designed based on their structural similarity to terpyridines. Four novel compounds 4a–d were synthesized by cyclization of amide de-rivatives of 3-aminopyridin-2(1H)-ones using pyridine-2,6-dicarboxylic acid and its di-chloride as key acidic components. Their structures and purity were confirmed by melt-ing point analysis, high-resolution mass spectrometry, and detailed 1H NMR spectros-copy. Photophysical studies in chloroform, dichloromethane, and acetonitrile revealed that compounds 4a–c exhibit intense blue to deep blue fluorescence (л_max 323–347 nm) with high quantum yields (φi ≈ 0.32–0.84), attributed to р–π* transitions within the con-jugated ring system. These findings suggest their potential as air-stable phosphors for organic electronics. Computational modeling of 4a–c molecules provided insight into their electronic structures, conformational stability, and predicted optical behavior. The most stable conformers (4a–II, 4b–II, 4c–II′) showed decreasing HOMO–LUMO gaps and photoactivity from 4a to 4c, with 4a–II emerging as the most promising fluorophore due to its high symmetry and consistent emission. Overall, this study lays the foundation for future studies of bis(oxazolo[5,4-b]pyridine) derivatives in coordination chemistry and optoelectronic materials development.

Abstract:

This review provides an integrated analytical overview of the phenolic constituents of Solenostemma argel, with emphasis on extraction efficiency, structural characterization, and antioxidant-linked bioactivity. Because direct studies on argel phenolics remain limited, a broadened inclusion strategy was adopted. Studies were considered when phenolic-solubilizing solvents were used, when antioxidant-related biological effects (such as antidiabetic, anticancer, or neuroprotective activities) were evaluated, or when chromatographic and spectroscopic techniques applicable to phenolic analysis were employed. Comparative findings indicate that moderately polar solvents—particularly ethanol, methanol, and acetone—produce the highest phenolic yields, especially under ultrasound- or microwave-assisted extraction conditions. Reported variations in total phenolic content (TPC) primarily reflect methodological differences; however, higher TPC values consistently correlate with stronger antioxidant activity across assays. Advanced analytical platforms, including HPLC and NMR, provide the highest accuracy for qualitative and quantitative characterization of major phenolic classes. Overall, this expanded review synthesizes current evidence on phenolic profiling, extraction methodologies, analytical applicability, and antioxidant potential of S. argel, underscoring the plant’s promise as a rich and underexplored source of bioactive phenolic compounds.

Abstract: Cocoa bean shells (CBS) represent a significant by-product of the transformation of cocoa beans, constituting approximately 15% of the total cocoa bean weight. Recently, interest in exploring the potential of these shells as a sustainable source of functional ingredients for use in cosmetics and nutraceuticals has grown. The present study investigates Microwave-Assisted Subcritical Water Extraction (MASWE) as a green and fast technique to recover bioactive compounds from CBS. A flash extraction (five minutes) at 170°C yielded a maximum of 45.79 mg of gallic acid equiva-lents (GAE) per gram of CBS, which was higher than that obtained using conventional conditions (25.73 mgGAE/gCBS with 50% acetone solution). Additionally, the HPLC pro-file of the extract from MASWE revealed a significant increase in hydroxybenzoic acids and catechin, compared to the conventional extract. Following the optimization of the extraction process, seven distinct resins were examined to isolate a bioactive-enriched fraction: Sepabeads SP700 was found to be the most effec-tive resin for concentrating such compounds, increasing both methylxanthines and TPC selectivity up to 4.2-fold. This valorization approach integrating MASWE and downstream optimization offers an innovative strategy to recover added-value products in line with green extraction and nutraceutical innovation.

Abstract:

Background/Objectives: Diabetes is a chronic metabolic disorder that leads to elevated blood sugar levels and has become a global concern. Though there has been an increase and evolution of antidiabetic drugs and therapeutics, they fall short of the desired efficacy and are often associated with adverse effects. This study explores reduced chalcone as a scaffold to design and synthesize potential antidiabetic drugs with improved efficacy through glycosylation and supplemented by in silico evaluation. Methodology: The 3ʹ-hydroxychalcone was initially reduced to 1-phenyl-3-(3ʹ-hydroxyphenyl)propane (2), followed by direct C-glycosylation at C-4ʹ under temperature control from -78 ℃ to room temperature (RT) and afforded the C-4ʹ glucosylated 1,3-diaryl propane. The first step in the mechanism was 3ʹ-O-glycosylation, and the resultant 3ʹ-O-a,b-glucose isomer mixture was isolated at -40 ℃. NMR spectroscopy and mass spectrometry were used to characterise and validate compound structures. These compounds' antidiabetic potentials and drug-likeness were evaluated through integrated computational techniques. Results: The main compound (5) showed no inhibitory activity against α-glucosidase and α-amylase. However, all the compounds showed higher probable antidiabetic activities and improved drug-likeness relative to aspalathin. Their binding affinity assessment showed they are potential ‘pan-binders’ with high binding affinities to several proteins implicated in the advancement of diabetes, including AKT, AMPK, GLUT4, SGLT2, and SIRT6. Furthermore, they were observed to stabilise within the binding pocket of AKT, underscored by strong hydrogen and hydrophobic bonds resulting in protein conformational changes, thus highlighting their antidiabetic potential. Conclusion: The synthesised glucosyl chalcones could be potential lead compounds for developing novel antidiabetic compounds.

Abstract: Natural products have and continue to be a remarkable resource, rich in structural di-versity, and endowed with valuable chemical and biological properties that have ad-vanced both science and society. Some natural products, especially those from marine organisms, are chemically reactive, and during extraction and handling can partially or totally transform into artifacts. All too often overlooked or mischaracterised as natural products, artifacts can be invaluable indicators of a uniquely evolved and primed chemical space, with enhanced chemical and biological properties highly prized for drug discovery. To demonstrate this potential, we review a wide selection of marine and mi-crobial case studies, revealing the factors that initiate artifact formation (e.g. solvents, heat, pH, light and air oxidation) and commenting on the mechanisms behind artifact for-mation. We conclude with reflections on how to recognise and control artifact formation, and how to exploit knowledge of artifacts as a window into unique regions of natural product chemical space — to better inform the development of future marine bioproducts.

Abstract: Pestasulfamides A and B are phenylbenzene-sulfonamides with an eight-membered dilactam, produced by mangrove endophytic fungus Pestalotiopsis sp. HNY36-1D. Herin, the first total synthesis of pestasulfamides A and B was achieved through one-pot protocol. The key step features an iminoketene dimeriazation of anthranilic acid triggered by a sulfonylation in a pyridine/THF system.

Abstract: The first representative of the aziridine-fused benzo[e][1,4]thiazine series was synthesized from methyl 2-bromo-2-phenyl-2H-azirine-2-carboxylate and benzo[d]thiazole in 74% yield. The reaction proceeds via the SN2’-SN2’-cascade to form the azirinylthiazolium salt followed by a water-induced thiazole ring expansion. The structure of the title compound was established based on 1H, 13C, 2D NMR spectroscopy, high-resolution mass spectrometry, and unambiguously confirmed by X-ray diffraction analysis.

Abstract: Synthesizing natural substances has always been a significant challenge for organic chemists. The key to a successful total synthesis lies in utilizing reactions that generate molecular complexity with high stereocontrol. Photochemical reactions offer immense potential in this regard, though their complex mechanisms require careful mastery. This review explores recent examples from the literature where light-mediated reactions are crucial, often irreplaceable by thermal alternatives. The manuscript is organized by dif-ferent photochemical processes, each introduced with relevant background. This review does not offer a complete analysis of all recent light-assisted syntheses; rather, it offers a glimpse into the growing trend of using photo-driven transformations to address signifi-cant synthetic challenges.

Abstract: The rapid adaptation of microorganisms to antibiotics, including those previously re-garded as last-resort choices, led to intractable superbugs among both Gram-positive and Gram-negative species, causing increasing antibiotic resistance (AR). AR triggers the worldwide propagation of tenacious to lethal infections, which need urgent development of novel antibacterial agents, active also on worrying superbugs. To this end, totally inac-tive betulin (BET) and betulinic acid (BA), as well as ursolic acid (UA) already active on bacteria Gram-positive, have been chemically modified achieving derivatives 1-7. Com-pounds 1 and 4-7 contained the triphenyl phosphonium (TPP) group, promoting antibac-terial effects, while 2 and 3 did not. 1-7 and all synthetic intermediates were characterized by, chemometric-assisted FTIR and NMR spectroscopy, as well as by other analytical techniques, which confirmed their structure and high purity. Determinations of the min-imum inhibitory concentration values (MICs) of 1-7, BET, BA and UA using a selection of Gram-positive and Gram-negative clinically isolated superbugs, evidenced that com-pounds 4-7 had potent antibacterial effects against Gram-positive strains, higher than those reported so far for other BET, BA and UA derivatives, mainly considering the com-plex pattern of resistance of isolates used here and their clinical source. For the first time, due to the use of TPP, a real activity (MICs 2-16 µg/mL) was conferred to inactive BET and BA (original MICs > 1024 and 256 µg/mL). Moreover, the antibacterial effects of UA were 16 and 32-fold improved against MRSE and MRSA (MICs = 2 vs. 23 and 64 μg/mL). These early, but very promising microbiologic results, pave the way for further experiments with the best performant compounds 5 and 7 (MICs = 2 μg/mL) on an enlarged number of Gram-positive isolates, to assess their time-killing curves, to evaluate their cytotoxicity on eukaryotic cells and to assess their possible antibiofilm activity.

Abstract: The epoxidation of 2,7-diaminooct-4-enedioic acid derivatives with different steric requirements at the homoallylic positions has been studied. Four readily available unsaturated bis-amino esters were used as model substrates for the synthesis of 2,7-diamino-4,5-epoxysuberic esters. The study revealed a reduced reactivity of all the unsaturated compounds towards epoxidation, but particularly of the most crowded one. Moderate stereoselectivity was observed in the epoxidation of C₂-symmetric chiral unsaturated bis-a-amino esters. All substrates were converted to the corresponding epoxides in high yields using an excess of Oxone^®/acetone.

Abstract: The reaction of a 2-naphthol-derived Mannich base with the push–pull 5-morpholinopenta-2,4-dienal under acidic conditions unexpectedly afforded (7aR*,7bR*)-7a,7b-dihydro-15H-dibenzo[f,f']cyclopenta[1,2-b:5,4-b']dichromene. The structure of this product was unambiguously confirmed by NMR spectroscopy and X-ray diffraction analysis. A plausible mechanism involves the in situ generation of 1,2-naphthoquinone-1-methide, followed by a [4 + 2] cycloaddition and a subsequent interrupted iso-Nazarov cyclization. In this process, the enol tautomer of the resulting fused cyclopentenone is trapped by a second equivalent of the 1,2-naphthoquinone-1-methide, leading to the observed polycyclic framework.