Macrocyclic peptidomimetics with antimicrobial activity: synthesis, bioassay, and molecular modeling studies

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dc.authoridGirgis, Adel S./0000-0003-4407-9745
dc.authoridPillai, Girinath G./0000-0003-3770-9585
dc.authoridPanda, Siva/0000-0003-3668-104X
dc.authoridTamm, Kaido/0000-0002-7401-4435
dc.authoridKucukbay, Fatumetuzzehra/0000-0001-7784-4138
dc.authoridElagawany, Mohamed/0000-0002-1597-5324
dc.authorwosidkucukbay, fatumetuzzehra/X-5743-2019
dc.authorwosidGirgis, Adel S./AFK-3725-2022
dc.authorwosidPillai, Girinath G./C-6459-2009
dc.authorwosidPanda, Siva/E-7856-2014
dc.authorwosidTamm, Kaido/A-6505-2013
dc.authorwosidElagawany, Mohamed/P-9626-2018
dc.contributor.authorIbrahim, Mohamed A.
dc.contributor.authorPanda, Siva S.
dc.contributor.authorOliferenko, Alexander A.
dc.contributor.authorOliferenko, Polina V.
dc.contributor.authorGirgis, Adel S.
dc.contributor.authorElagawany, Mohamed
dc.contributor.authorKucukbay, F. Zehra
dc.date.accessioned2024-08-04T20:41:10Z
dc.date.available2024-08-04T20:41:10Z
dc.date.issued2015
dc.departmentİnönü Üniversitesien_US
dc.description.abstractNovel, cyclic peptidomimetics were synthesized by facile acylation reactions using benzotriazole chemistry. Microbiological testing of the synthesized compounds revealed an exceptionally high activity against Candida albicans with a minimum inhibitory concentration (MIC) two orders of magnitude lower than the MIC of the antifungal reference drug amphotericin B. A strikingly high activity was also observed against three Gram-negative bacterial strains (Pseudomonas aeruginosa, Klebsiella pneumoniae and Proteus vulgaris), two of which are known human pathogens. Thus the discovered chemotype is a potential poly-pharmacological agent. The toxicity against mammalian tumor cells was found to be low, as demonstrated in five different human cell lines (HeLa, cervical; PC-3, prostate; MCF-7, breast; HepG2, liver; and HCT-116, colon). The internal consistency of the experimental data was studied using 3D-pharmacophore and 2D-QSAR.en_US
dc.description.sponsorshipUniversity of Florida, United States; Kenan Foundationen_US
dc.description.sponsorshipWe thank the University of Florida, United States and the Kenan Foundation for financial support.en_US
dc.identifier.doi10.1039/c5ob01400j
dc.identifier.endpage9503en_US
dc.identifier.issn1477-0520
dc.identifier.issn1477-0539
dc.identifier.issue36en_US
dc.identifier.pmid26256838en_US
dc.identifier.scopus2-s2.0-84940851334en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage9492en_US
dc.identifier.urihttps://doi.org/10.1039/c5ob01400j
dc.identifier.urihttps://hdl.handle.net/11616/96967
dc.identifier.volume13en_US
dc.identifier.wosWOS:000360656100019en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherRoyal Soc Chemistryen_US
dc.relation.ispartofOrganic & Biomolecular Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAnti-Oncological Alkaloidsen_US
dc.subjectRegioselective Synthesisen_US
dc.subjectRational Designen_US
dc.subjectAmphotericin-Ben_US
dc.subjectQsaren_US
dc.subjectDerivativesen_US
dc.subjectPeptidesen_US
dc.subjectEfficacyen_US
dc.subjectSpectrumen_US
dc.titleMacrocyclic peptidomimetics with antimicrobial activity: synthesis, bioassay, and molecular modeling studiesen_US
dc.typeArticleen_US

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