Synthesis of Benzimidazole-1,2,4-triazole Derivatives as Potential Antifungal Agents Targeting 14α-Demethylase

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dc.authoridEVREN, Asaf Evrim/0000-0002-8651-826X
dc.authoridKAYIS, UGUR/0000-0003-0020-0857
dc.contributor.authorGuzel, Emir
dc.contributor.authorCevik, Ulviye Acar
dc.contributor.authorEvren, Asaf Evrim
dc.contributor.authorBostanci, Hayrani Eren
dc.contributor.authorGul, Ulkuye Dudu
dc.contributor.authorKayis, Ugur
dc.contributor.authorOzkay, Yusuf
dc.date.accessioned2025-05-04T16:46:58Z
dc.date.available2025-05-04T16:46:58Z
dc.date.issued2023
dc.departmentSivas Cumhuriyet Üniversitesi
dc.description.abstractInvasive fungal infections (IFIs) are increasing as major infectious diseases around the world, and the limited efficacy of existing medications has resulted in substantial morbidity and death in patients due to the lack of effective antifungal agents and serious drug resistance. In this study, a series of benzimidazole-1,2,4-triazole derivatives (6a-6l) were synthesized and characterized by 1H NMR, 13C NMR, and HR-MS spectral analysis. All the target compounds were screened for their in vitro antifungal activity against four fungal strains, namely, C. albicans, C. glabrata, C. krusei, and C. parapsilopsis. The synthesized compounds exhibited significant antifungal potential, especially against C. glabrata. Three compounds (6b, 6i, and 6j) showed higher antifungal activity with their MIC values (0.97 mu g/mL) compared with voriconazole and fluconazole. Molecular docking provided a possible binding mode of compounds 6b, 6i, and 6j in the 14 alpha-demethylase active site. Our studies suggested that the benzimidazole-1,2,4-triazole derivatives can be used as a new fungicidal lead targeting 14 alpha-demethylase for further structural optimization. In addition, their effects on the L929 cell line were also investigated to evaluate the cytotoxic effects of the compounds. SEM analyses were performed to examine the effects of compounds 6a, 6i, and 6j on C. glabrata cells under in vivo experimental conditions.
dc.identifier.doi10.1021/acsomega.2c07755
dc.identifier.endpage4384
dc.identifier.issn2470-1343
dc.identifier.issue4
dc.identifier.pmid36743066
dc.identifier.scopus2-s2.0-85146728330
dc.identifier.scopusqualityQ1
dc.identifier.startpage4369
dc.identifier.urihttps://doi.org/10.1021/acsomega.2c07755
dc.identifier.urihttps://hdl.handle.net/20.500.12418/35436
dc.identifier.volume8
dc.identifier.wosWOS:000923270500001
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherAmer Chemical Soc
dc.relation.ispartofAcs Omega
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/openAccess
dc.snmzKA_WOS_20250504
dc.subjectCandida
dc.subjectDrug
dc.titleSynthesis of Benzimidazole-1,2,4-triazole Derivatives as Potential Antifungal Agents Targeting 14α-Demethylase
dc.typeArticle

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