Multicomponent reactions effectively contribute to modern organic and medicinal chemistry. 4-Thiazolidinone core and cyclopropyl moiety are important structural motifs for design of potential biologically active molecules. In the present paper, the convenient step-economy and cost-effective synthesis of 2-(cyclopropylamino)-5-(4-methoxybenzylidene)thiazol-4(5H)-one (2) is described based on the application of the MCR methodology. The proposed approach includes direct one-pot interaction of 2-thioxothiazolidin-4-one (rhodanine), 4-methoxybenzaldehyde with cyclopropylamine which was used in 10% excess compare to other reagents. The structure of synthesized compound 2 was confirmed using ¹H, ¹³C, 2D NMR, LC-MS, IR and UV spectra. The presence of prototropic amino/imino tautomerism for synthesized compound 2 was observed based on spectral analysis data. Screening of antimicrobial activity against 12 strains of Gram-positive and Gram-negative bacteria, as well as yeasts, was performed for synthesized derivative 2. © 2022 by the authors.

УДК 579.86:[616.98:362.11]

In the Lviv region, cases of healthcare-associated infections (HAIs) in children occur, but are practically not registered. For the period 2019–2021, not a single case was registered. Purpose — to identify and compare the species composition of potential HAIs pathogens in children and adults in Lviv hospitals. Materials and methods. Material for the study was collected from children from various biological niches who were undergoing inpatient treatment in Lviv hospitals. Identification was carried out using MIKRO-LA-TEST kits manufactured by Erba Lachema. Antibiotic susceptibility was determined according to EUCAST recommendations. Results. Among the isolated gram-positive microbiota that meets the criteria of HAIs, enterococci were most often detected in adults (30,8%), among children (from 0 to 17 years) — in 35,4% of cases. Staphylococcus epidermidis was detected in 21,5% from children's patients, as the causative agent of the purulent-septic process, while in adults – 27,2%. A significant part of S. aureus cultures (63,6%) isolated from children was resistant to amoxicillin (among adults — 56,5%), ceftazidime (54,5%) and cefuroxime (45,4%). Among adult patients, the percentage of isolated resistant strains to ceftriaxone (65,2%), cefotaxime (52,2%), cefepime (87,0%) was significantly higher compared to such indicators in children – 9,1%, 18,2% and 36,4%. The antibiotic ceftizoxime, widely used in recent years in the treatment of children, was not effective in 45,5% of cases. Conclusions. Despite the low level of registration of HAIs in children, this problem exists. The number of resistant strains is increasing. The sensitivity of strains to antibiotics isolated in children and adults differs significantly, so general recommendations may not be effective. The role of the clinical microbiologist and epidemiologist is extremely important for effective infection control and quality empiric antibiotic therapy in individual healthcare settings. The research was carried out in accordance with the standarts of bioethics, approved by the ethics committee of the Danylo Halytskyi LNMU. The informed consent of the child's parents and the patient was obtained for the description of the clinical case. © 2023 Group of Companies Med Expert, LLC. All rights reserved.

Introduction: Research among the Ukrainian (Carpatian) floras representatives is important for searching for new active compounds. Objective: The study aims to determine the potential of callus biomass of Delphinium elatum, Anemone nemorosa, and Pulsatilla alba to become an analog of medicinal plant raw material for the use in the pharmaceutical industry, to investigate the composition, antioxidant activity and antimicrobial activity of extracts of the callus biomass of the above-mentioned plants. Methods: The individual members of the family Ranunculaceae (Delphinium elatum L., Anemone nemorosa L., Pulsatilla alba Rchb.) were introduced into in vitro culture, and their callus induction was studied using the Folin-Ciocalteu spectrophotometric method, colorimetric analysis, antioxidant, and antimicrobial activity methods. Results: The maximum content of flavonoids and phenolic compounds was observed in 40% hydro-ethanolic extracts of callus biomass and plant raw materials of D. elatum. 90.0% and 70.0% D. elatum extracts showed significant activity against Gram-positive microorganisms. 90.0/70.0/40.0% extracts showed significant activity against Bacillus licheniformis. 70.0 % extract showed significant antifungal activity against clinical and reference strains of Candida albicans. Conclusion: Summarizing experimental results, it was proved that the callus biomass of D. elatum, A. nemorosa, and P. alba have potential as analogs of medicinal plant raw materials, both for the content of biologically active substances and biological activities. © 2023 Sciendo. All rights reserved.

UDC 547-327:547.821:54.057

The aim. The combination in one molecule of pharmacophore fragments of thieno[2,3-d]pyrimidine-4-carboxylic acids with the fragments of 2-or 4-aminopyrimidine by peptide coupling promoted acylation in order to develop the new drug-like molecules with antimicrobial activity. Materials and methods. The molecular docking studies were performed with the AutoDock Vina and AutoDock-Tools 1.5.6 programs; TrmD Pseudomonas aeruginosa PDB ID – 5ZHN was used as the protein target. Synthetic methods of peptide coupling were used. 1H and 13C NMR spectra were recorded with a Varian-400 spectrometer at 400 MHz and Bruker Avance DRX 500 device at 500 MHz and 125 MHz in DMSO-d6 as a solvent, using TMS as the internal standard. LC-MS analysis of the compounds was carried out with Agilent 1100 HPLC з with at-mospheric pressure chemical ionization (APCI). The studied derivates were tested in vitro for their antibacterial and anti-fungal activities using agar diffusion and serial dilutions resazurin-based microdilution assays (RBMA). Results and discussion. By the combination of the pharmacophore fragments of thieno[2,3-d]pyrimidine-4-carboxylic acids with the fragments of 2-of 4-aminopyrimidine, the combinatorial library of amides was constructed. For this library of compounds, the potential of antimicrobial activity was revealed using docking studies to the TrmD enzyme isolated from P. aeruginosa. The peptide coupling promoted by 1,1’-carbonyldiimidazole was found to be effective for the synthesis of pyridyl amides of thieno[2,3-d]pyrimidine-4-carboxylic acids, and it allowed to combine these phar-macophores in one molecule. The results of antimicrobial activity study revealed the broad spectrum of antimicrobial activity for N-(pyridin-4-yl)-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidine-4-carboxamide (2g), while 5,6-di-methyl-N-(6-methylpyridin-2-yl)thieno[2,3-d]pyrimidine-4-carboxamide (2c) showed the best MIC value against the reference strain of Pseudomonas aeruginosa ATCC 10145. N-(6-Methylpyridin-2-yl)-5,6,7,8-tetrahydro[1]benzothien-o[2,3-d]pyrimidine-4-carboxamide (2h) was also found to be active against Pseudomonas aeruginosa. Conclusions. An effective method for the synthesis of pyridyl amides of thieno[2,3-d]pyrimidine-4-carboxylic acid has been developed. The amides molecular docking method showed their ability to inhibit TrmD enzyme isolated from P. aeruginosa; the further in vitro studies of the compounds showed the rationality of the further studies of the derivatives with 2-ami-no-6-methylpyridine in amide substituent because this fragment favoured the selectivity against Pseudomonas aeruginosa. © The Author(s) 2023.

The analysis presented in this article is a continuation of a broader qualitative study examining the composition of the chloroform fraction of Caltha palustris. The study discovered 29 compounds, and 26 of them have been identified:paraffinic hydrocarbons, esters, fatty aldehydes, morphine derivatives, thiazole derivatives, benzodiazepines, naphthalene, and a small amount of terpene. It was figured out that the investigated lipophilic extract has an antioxidant impact. For the investigation, there were used such assays as the DPPH radical and the ABTS radical cation assays. Moreover the investigated lipophilic extract has an antimicrobial activity both in terms of gram-positive (Staphylococcus aureus (ATCC 25923 (F-49)), Bacillus cereus 34 (non-MDR), Enterococcus faecalis 26(MDR) and gram-negative, (Raoultella terrigena (ATCC 33257), Escherichia coli (ATCC 25922), Escherichia coli 168) microorganisms and yeast Candida spp. In addition, the significant content of biologically active substances in the lipophilic volatile fraction of Caltha palustris indicates the prospects for further study. © 2023, Research Journal of Pharmacy and Technology. All rights reserved.