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The Synthesis and Evaluation of Aminocoumarin Peptidomimetics as Cytotoxic Agents on Model Bacterial E. coli Strains

2021; Multidisciplinary Digital Publishing Institute; Volume: 14; Issue: 19 Linguagem: Inglês

10.3390/ma14195725

1996-1944

Paweł Kowalczyk, Monika Wilk, Parul Sahrawat, Mateusz Szymczak, Karol Kramkowski, S. Raj, G. Skiba, Dorota Sulejczak, Patrycja Kleczkowska, Ryszard Ostaszewski,

Chemical Synthesis and Analysis

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.