The Synthesis and Evaluation of Aminocoumarin Peptidomimetics as Cytotoxic Agents on Model Bacterial E. coli Strains
| Autor: | Patrycja Kleczkowska, Paweł Kowalczyk, Parul Parul, Monika Wilk, Grzegorz Skiba, Stanisława Raj, Ryszard Ostaszewski, Karol Kramkowski, Dorota Sulejczak, Mateusz Szymczak |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Technology
Peptidomimetic Ugi multicomponent reaction Fpg protein-formamidopyrimidine Aldehyde Article chemistry.chemical_compound Benzylamine Biological property oxidative stress General Materials Science heterocyclic compounds Cytotoxicity chemistry.chemical_classification Microscopy QC120-168.85 Trifluoromethyl Chemistry QH201-278.5 Coumarin Antimicrobial coumarin derivatives Engineering (General). Civil engineering (General) Combinatorial chemistry TK1-9971 Descriptive and experimental mechanics Electrical engineering. Electronics. Nuclear engineering TA1-2040 DNA-N-glycosylase lipopolysaccharide (LPS) |
| Zdroj: | Materials, Vol 14, Iss 5725, p 5725 (2021) Materials Volume 14 Issue 19 |
| ISSN: | 1996-1944 |
| Popis: | This work presents the successful synthesis of a library of novel peptidomimetics via Ugi multicomponent reaction. Most of these peptidomimetics contain differently substituted aminocoumarin 7-amino-4-methylcoumarin and 7-amino-4-(trifluoromethyl) coumarin. Inspired by the biological properties of coumarin derivatives and peptidomimetics, we proposed the synthesis of coumarin incorporated peptidomimetics. We studied the potential of synthesized compounds as antimicrobial drugs on model E. coli bacterial strains (k12 and R2–R4). To highlight the importance of coumarin in antimicrobial resistance, we also synthesized the structurally similar peptidomimetics, using benzylamine. Preliminary cellular studies suggest that the compounds with coumarin derivatives have more potential as antimicrobial agents compared to the compounds without coumarin. We also analyzed the effect of aldehyde, free acid group and ester group on the course of their antimicrobial properties. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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