UDC: 615.276:547.789:542.91

Aim. Based of the Knoevenagel condensation reaction the synthesis of new rhodanine-indoline hybrid molecules for screening antibacterial and antifungal activities was accomplished. Methods. Organic synthesis, NMR spectroscopy, pharmacological screening. Results. The reaction between rhodanine-3-propanoic/ethanesulfonic acids and indolecarbaldehydes in the acetic acid provided series of 5-indolylmethylenerhodanine-3-carboxylic/sulfonic acid deriva-
tives. Based on the esterification reaction with methanol in the presence of sulfuric acid, 5-indolylmethylenerhodanine-3-propanic acid was transformed into appropriate ester for further evaluation of antimicrobial activity. The antimicrobial activity screening allowed the identification of compounds with significant effect against Escherichia coli, Staphylococcus lentus and Candida albicans with MIC/MBC/MFC values in the range of 25-50 μg/mL.
Conclusions. The synthesized 5-indolylmethylenerhodanine-3-carboxylic/sulfonic acid derivatives are a convenient platform for the development of new highly active and low-toxic agents as potential drug-like molecules with antimicrobial activity.
K e y w o r d s: synthesis, 2-thioxo-4-thiazolidinone, indolecarbaldehydes, spectral data, antimicrobial activity.

УДК 582.94 + 615.28 + 615.32

Ключові слова: Phlomis pungens, наночастинки срібла, спрей, антибактеріальна дія.
У статті представлено результати досліджень Phlomis pungens та екстрактів на його основі. Підібрано оптимальні умови одержання екстрактів та визначено кількісний вміст біологічно активних речовин у них, а саме фенольних сполук і флавоноїдів. Вивчено фармакологічну активність екстрактів рослини та наночастинок срібла. Розроблено склад та досліджено новий антисептичний засіб у формі спрею на основі екстракту Phlomis pungens та наночастинок срібла.

УДК: 615.23/.32:339.146

Ключові слова: Ficaria verna, Ranuncul aceae, поширення, ботанічний опис, вміст біологічно активних речовин, застосування.
У статті представлено результати аналізу джерел літератури та узагальнення даних щодо ботанічного опису, ареалу поширення, хімічного складу, фармакологічної дії та особливостей використання Ficaria verna у фармації та медицині. Базуючись на результатах дослідження встановлено перспективи проведення ґрунтовних фармакогностичних, фітохімічних та фармакологічних досліджень рослини.

UDC 615.276:547.789:542.91

Aim. The screening of antimicrobial and cytotoxic activities of thiazolo[4,5-b]pyridine derivatives was accomplished. Methods. The antibacterial and antifungal activities of synthesized thiazolopyridines were evaluated in vitro with the agar diffusion and broth microdilution methods using clinical and reference strains of Gram-positive, Gram-negative bacteria and yeasts. The structure-antibacterial/antifungal activity relationships of the screened compounds were established. The target compounds were screened for their cytotoxicity effects on HaCaT and HEK293 cells using MTT assay. Results. The highest antimicrobial activity was observed for compound V 2-oxo-7-thiophen-2-yl-2,3-dihydrothiazolo[4,5-b]pyridine-5-carboxylic acid with minimal inhibitory concentration (MIC) 12.5 μg/mL against Candida albicans. At the same time, the synthesized compounds were explored in the interaction with amoxicillin against multidrug resistant clinical isolates of ESβL+ Klebsiella pneumonie and Staphylococcus haemolyticus (MRSH). The best synergistic activity with amoxicillin was exhibited by compound VI. HaCaT human keratinocytes and HEK293 human embryonic kidney cells demonstrated resistance to the thiazolopyridine derivatives treatment and did not reach the IC50 value up to 100 µM. Conclusions. The tested thiazolopyridines constitute an interesting background for further development of new chemotherapeutic agents. K e y w o r d s: heterocyclic compounds, thiazolidinones, thiazolo[4,5-b]pyridines, antimicrobial activity, antiproliferative activity

UDC: 615.276:547.789:542.91

Aim. To accomplish the synthesis and screening of anticancer and antimicrobial activities of 1-[2-amino-4-methylthiazol-5-yl]-3-arylpropenones 2-10. Methods. The in vitro anticancer activity of compounds 4, 6, 8-10 has been established by DTP(Developmental Therapeutics Program) of the National Cancer Institute. The antibacterial and antifungal activities of synthesized thiazole-based derivatives were evaluated in vitro with the agar diffusion and broth microdilution methods to wards Gram-positive, Gram-negative bacteria and yeasts. For the synthesized compounds, the in silico drug-likeness screening using SwissADME online server is reported. Results. The novel 1-[2-amino-4-methylthiazol-5-yl]-3-arylpropenones were synthesized from 1-[2-amino-4-methylthiazol-5-yl]ethanones and various aromatic aldehydes in the Claisen–Schmidt condensation. The synthesized compound 9 was moderately active
against the leukemia CCRF-CEM and HL-60(TB), renal cancer UO-31 and breast cancer MCF7 cell lines. The antimicrobial screening led to identification of the active compound 10 against Staphylococcus aureus, Pseudomonas aeruginosa, and Candida albicans. Conclusions. The results obtained herein provide a platform for structure-based optimization of these newly identified thiazole-based compounds for the anticancer and antibacterial drug design. K e y w o r d s: thiazoles, Claisen-Schmidt condensation, anticancer activity, antimicrobial activity, SwissADME