Influence of Open Chain and Cyclic Structure of Peptidomimetics on Antibacterial Activity in E. coli Strains

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dc.contributor.authorSahrawat, Parul
dc.contributor.authorKowalczyk, Paweł
dc.contributor.authorKoszelewski, Dominik
dc.contributor.authorSzymczak, Mateusz
dc.contributor.authorKramkowski, Karol
dc.contributor.authorWypych, Aleksandra
dc.contributor.authorOstaszewski, Ryszard
dc.contributor.editorSilva, Artur M. S.
dc.contributor.organizationInstitute of Organic Chemistry, Polish Academy of Sciencesen
dc.contributor.organizationThe Kielanowski Institute of Animal Physiology and Nutrition, Polish Academy of Sciencesen
dc.contributor.organizationInstitute of Microbiology, University of Warsawen
dc.contributor.organizationDepartment of Physical Chemistry, Medical University of Bialystoken
dc.contributor.organizationCentre for Modern Interdisciplinary Technologies, Nicolaus Copernicus University in Torunen
dc.date.accessioned2022-08-31T12:02:29Z
dc.date.available2022-08-31T12:02:29Z
dc.date.issued2022
dc.description.abstractAn efficient method for the synthesis of functionalized peptidomimetics via multicomponent Ugi reaction has been developed. The application of trifluoroethanol (TFE) as a reaction medium provided desired products with good yields. Further, using the developed cyclisation reaction, the obtained peptidomimetics were transformed into the cyclic analogues (diketopiperazines, DKPs). The goal of the performed studies was to revised and compare whether the structure of the obtained structurally flexible acyclic peptidomimetics and their rigid cycling analogue DKPs affect antimicrobial activity. We studied the potential of synthesized peptidomimetics, both cyclic and acyclic, as antimicrobial drugs on model E. coli bacteria strains (k12, R2–R4). The biological assays reveal that DKPs hold more potential as antimicrobial drugs compared to open chain Ugi peptidomimetics. We believe that it can be due to the rigid cyclic structure of DKPs which promotes the membrane penetration in the cell of studied pathogens. The obtained data clearly indicate the high antibiotic potential of synthesized diketopiperazine derivatives over tested antibiotics.en
dc.description.sponsorshipMedical University of Białystok SUB/2/DN/22/001/2201 National Science Centre, project OPUS No. 2019/33/B/ST4/01118
dc.identifier.citationSahrawat, P.; Kowalczyk, P.; Koszelewski, D.; Szymczak, M.; Kramkowski, K.; Wypych, A.; Ostaszewski, R. Influence of Open Chain and Cyclic Structure of Peptidomimetics on Antibacterial Activity in E. coli Strains. Molecules 2022, 27, 3633. https://doi.org/10.3390/molecules27113633en
dc.identifier.doi10.3390/molecules27113633
dc.identifier.issn1420-3049
dc.identifier.urihttps://open.icm.edu.pl/handle/123456789/21594
dc.language.isoen
dc.publisherMDPIen
dc.rightsUznanie autorstwa 4.0 Międzynarodowe*
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/*
dc.subjectcyclic peptideen
dc.subjectugi multicomponent reactionen
dc.subjectdiketopiperazinesen
dc.subjectantimicrobial activityen
dc.subjectminimal inhibitory concentrationen
dc.titleInfluence of Open Chain and Cyclic Structure of Peptidomimetics on Antibacterial Activity in E. coli Strainsen
dc.typearticleen
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