The interaction results of 1,2-dibromo-3-isothiocyanatopropane with some pyrazoles as well as cytisine and salsoline alkaloids were presented in this paper. It was shown that the reaction resulted in one one-step and rather mild method for the preparation of the corresponding 1,3-thiazoline bromomethyl derivatives. The yield of this reaction was affected by the presence of a base and an order in which reagents were added. Molecular docking of the synthesized 1,3-thiazoline derivatives for putative antibacterial activity was carried out using the penicillin-binding target protein (PBP4) of the bacteria E. coli “Homo sapiens” and S. aureus “Homo sapiens” as an example. Molecular docking demonstrated that the compounds had insignificant binding energies at the level of selected reference drugs (Cephalotin and Chloramphenicol). The presence of natural alkaloids in the structure of thiazoline derivatives somewhat increased the affinity of these substrates for target proteins selected.

Influenza is a disease of significant morbidity and mortality. The number of anti-influenza drugs is small; many of them stimulate the appearance of resistant strains. This article presents the results of assessing the antiviral activity of 1,2,3-triazole-containing derivatives of alkaloid lupinine for their ability to suppress the reproduction of orthomyxoviruses (influenza viruses: A/Vladivostok/2/09 (H1N1) and A/Almaty/8/98 (H3N2)). The ability of (1S,9aR)-1-[(1,2,3-triazol-1-yl)-methyl]octahydro-1H-quinolizines with aryl-, 4-((4-formylphenoxy)methyl)- or 4-((3-tert-butyl-5-ethyl-2-hydroxy-benzoyloxy)methyl)- substituents at the C-4 position of the triazole ring to reduce the infectivity of the virus when processing virus-containing material was established, indicating good prospects for the studied compounds as virucidal agents affecting extracellular virions. The experimental results demonstrated that the triazolyl lupinine derivatives exhibited varying degrees of affinity for both hemagglutinin and neuraminidase proteins. Furthermore, these compounds demonstrated inhibitory effects on the replication of influenza viruses with different antigenic subtypes. The obtained biological data are in agreement with the results of molecular docking, which showed strong binding energies of the investigated compounds under study with biological targets—hemagglutinin and neuraminidase proteins. Following the evaluation of antiviral efficacy among the studied triazolyl derivatives of lupinine, four compounds have been identified for subsequent comprehensive in vitro and in vivo investigations to further elucidate their antiviral properties.

A composite material based on polyvinyl alcohol (PVA) and hydroxyapatite modified with magnesium (0.3; 0.5; 1.0 mol) was developed using the in situ mineralization method. A thorough analysis confirmed the formation of a two-phase system, with a uniform distribution of HA particles within the PVA matrix. In addition, the analysis confirmed the successful incorporation of magnesium into the crystal lattice without the formation of secondary phases. The material exhibited a developed macroporous structure, with porosities ranging from 50 to 200 μm. In order to ensure that the rheological properties of the composition were suitable for 3D printing, 4 wt.% gelatin was added, resulting in stable scaffolds. In vitro studies demonstrated high biocompatibility of the materials and a synergistic effect of the components: PVA has been demonstrated to neutralise the cytotoxic effects of HA, while magnesium has been shown to statistically significantly increase the viability of macrophages. The combination of a polymer matrix with an inorganic phase results in a material that exhibits both elasticity and bioactivity. The structural and functional characteristics of these systems render them promising materials for tissue engineering, particularly for bone regeneration and the creation of biocompatible 3D scaffolds.

This article has studied the synthesis of a new derivative of the known alkaloid cytisine contained in the seeds of plants of Cytisus laburnum L. and Thermopsis lanceolata R.Br., both of the Lugiminosae family. The new compound has been obtained from two biologically active compounds, such as isoxazole and cytisine. It has been demonstrated that the reaction led to the single-stage method under very mild conditions to obtain 4-[(3,5-dimethyl-1,2-oxazol-4-yl)sulfonyl]cytisine. This class of compounds is promising for obtaining the new biologically active compounds. This article has examined, in detail, a structure with using the ¹H and ¹³C NMR and two-dimensional NMR spectroscopy of COSY (¹H-¹H), HMQC (¹H-¹³C) and HMBC (¹H-¹³C). As a result, the homo- and heteronuclear spin-spin couplings should be established. The X-ray diffraction analysis has determined the spatial structure of a new derivative based on the cytisine alkaloid. Thus, its hemorheological activity has been studied.

Mono and diesters of 2-vinyloxyethylcarbamodithioic acid were synthesized by the reaction of (1--nitrophenyl)-2-vinyloxyethylaminoethanol with carbon disulfide. 3-[2-(Vinyloxyethyl)]-5-(4-nitrophenyl)-1,3-thiazolidine-2-thione was prepared and its structure was proved by X-ray diffraction analysis.