Azole derivatives with naphthalene showing potent antifungal effects against planktonic and biofilm forms ofCandidaspp.: an in vitro and in silico study

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dc.authoridKarakurt, Arzu/0000-0003-2209-0871
dc.authoridSARI, SUAT/0000-0002-8248-4218
dc.authoridSARI, SUAT/0000-0002-8248-4218
dc.authoridOzdemir, Zenyep/0000-0003-4559-2305
dc.authoridKocak Aslan, Ebru/0000-0003-0191-0746
dc.authorwosidKarakurt, Arzu/ABH-9340-2020
dc.authorwosidSARI, SUAT/A-5249-2017
dc.authorwosidSARI, SUAT/JCD-8070-2023
dc.authorwosidKART, DIDEM/I-8446-2013
dc.authorwosidOzdemir, Zenyep/AAJ-6384-2020
dc.contributor.authorSari, Suat
dc.contributor.authorKocak, Ebru
dc.contributor.authorKart, Didem
dc.contributor.authorOzdemir, Zeynep
dc.contributor.authorAcar, M. Fahir
dc.contributor.authorSayoglu, Burcu
dc.contributor.authorKarakurt, Arzu
dc.date.accessioned2024-08-04T20:48:54Z
dc.date.available2024-08-04T20:48:54Z
dc.date.issued2021
dc.departmentİnönü Üniversitesien_US
dc.description.abstractCandidainfections pose a serious public health threat due to increasing drug resistance. Azoles are first-line antifungal drugs for fungal infections. In this study, we tested an in-house azole collection incorporating naphthalene ring to find hits against planktonic and biofilm forms of resistantCandidaspp. In the collection, potent derivatives were identified against the susceptible strains ofCandidawith minimum inhibitory concentration (MIC) values lower than those of the reference drug, fluconazole. MIC values of 0.125 mu g/ml againstC. albicans, 0.0625 mu g/ml againstC. parapsilosis, and 2 mu g/ml againstC. krusei, an intrinsically azole-resistant non-albicans Candida, were obtained. Some of the derivatives were highly active against fluconazole-resistant clinical isolate ofC. tropicalis. Inhibition ofC. albicansbiofilms was also observed at 4 mu g/ml similar as amphotericin B, the reference drug known for its antibiofilm activity. Through molecular docking studies, affinities and key interactions of the compounds with fungal lanosterol 14 alpha-demethylase (CYP51), the target enzyme of azoles, were predicted. The interactions of imidazole with heme cofactor and of the naphthalene with Tyr118 were highlighted in line with the literature data. As a result, this study proves the importance of naphthalene for the antifungal activity of azoles againstCandidaspp. in both planktonic and biofilm forms.en_US
dc.identifier.doi10.1007/s10123-020-00144-y
dc.identifier.endpage102en_US
dc.identifier.issn1139-6709
dc.identifier.issn1618-1905
dc.identifier.issue1en_US
dc.identifier.pmid32889579en_US
dc.identifier.scopus2-s2.0-85090449640en_US
dc.identifier.scopusqualityQ3en_US
dc.identifier.startpage93en_US
dc.identifier.urihttps://doi.org/10.1007/s10123-020-00144-y
dc.identifier.urihttps://hdl.handle.net/11616/99525
dc.identifier.volume24en_US
dc.identifier.wosWOS:000566322700001en_US
dc.identifier.wosqualityQ3en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherSpringeren_US
dc.relation.ispartofInternational Microbiologyen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectNaphthaleneen_US
dc.subjectAntifungalen_US
dc.subjectCandidaen_US
dc.subjectBiofilmen_US
dc.subjectMolecular dockingen_US
dc.titleAzole derivatives with naphthalene showing potent antifungal effects against planktonic and biofilm forms ofCandidaspp.: an in vitro and in silico studyen_US
dc.typeArticleen_US

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