The Knoevenagel reaction is an essential synthetic tool in the organic and medicinal chemistry of thiazolidin-4-one derivatives. In the present work, the application of ethylenediamine diacetate (EDDA) as an effective catalyst for the interaction of 2-thioxothiazolidin-4-one with 4-(tert-butyl)cyclohexanone is proposed. The structure of novel synthesized 5-[4-(tert-butyl)cyclohexylidene]-2-thioxothiazolidin-4-one (yield 61%) was confirmed by¹H-,¹³C-NMR, LC-MS, IR, and UV spectra. Drug-like properties of the synthesized compound were evaluated in silico using the SwissAdme, and their potential antimicrobial activity against 15 strains of Gram-positive and Gram-negative bacteria as well as yeasts was evaluated in vitro. The synthesized compound possesses satisfactory drug-like parameters and promising antimicrobial properties and presents interest as a prospective intermediate for the forthcoming design of biologically active small molecules. © 2021 by the authors. Licensee MDPI, Basel, Switzerland.

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.