Synthesis, Characterization and Bioassay of Novel Substituted 1-(3-(1,3-Thiazol-2-yl)phenyl)-5-oxopyrrolidines
| Autor: | Božena Šovkovaja, Eglė Mickevičiūtė, Jūratė Šiugždaitė, Birutė Sapijanskaitė-Banevič, Rita Vaickelionienė |
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| Přispěvatelé: | MDPI AG (Basel, Switzerland) |
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
Benzimidazole
Staphylococcus aureus Pyrrolidines Stereochemistry Bacillus cereus Pharmaceutical Science Oxadiazole biological activity Microbial Sensitivity Tests 010402 general chemistry medicine.disease_cause 01 natural sciences Article Analytical Chemistry lcsh:QD241-441 pyrrolidinones chemistry.chemical_compound Structure-Activity Relationship lcsh:Organic chemistry Drug Discovery medicine Escherichia coli Physical and Theoretical Chemistry Thiazole triazoles Pyrrole heterocycles Oxadiazoles biology Molecular Structure 010405 organic chemistry Organic Chemistry Biological activity biology.organism_classification Listeria monocytogenes 0104 chemical sciences Anti-Bacterial Agents Thiazoles chemistry Chemistry (miscellaneous) Molecular Medicine Organic synthesis thiazoles |
| Zdroj: | Molecules Molecules, Vol 25, Iss 2433, p 2433 (2020) Volume 25 Issue 10 Molecules, Basel : MDPI, 2020, vol. 25, iss. 10, art. no. 2433, p. 1-19 |
| ISSN: | 1420-3049 |
| Popis: | Thiazole derivatives attract the attention of scientists both in the field of organic synthesis and bioactivity research due to their high biological activity. In the present study, thiazole ring was obtained by the interaction of 1-(4-(bromoacetyl)phenyl)-5-oxopyrrolidine-3-carboxylic acid with thiocarbamide or benzenecarbothioamide, as well as tioureido acid. A series of substituted 1-(3-(1,3-thiazol-2-yl)phenyl)-5-oxopyrrolidines with pyrrolidinone, thiazole, pyrrole, 1,2,4-triazole, oxadiazole and benzimidazole heterocyclic fragments were synthesized and their antibacterial properties were evaluated against Gram-positive strains of Staphylococcus aureus, Bacillus cereus, Listeria monocytogenes and Gram-negative Pseudomonas aeruginosa, Escherichia coli and Salmonella enterica enteritidis. The vast majority of compounds exhibited between twofold and 16-fold increased antibacterial effect against the test-cultures when compared with Oxytetracycline. |
| Databáze: | OpenAIRE |
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