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Synthesis and molecular modeling of some novel hydroxypyrone derivatives as antidermatophytic agents

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dc.contributor.authorTÜRE, ASLI
dc.contributor.authorsKarakaya G., Ozdemir A., Ture A., ÖZÇELİK B., Aytemir M.
dc.date.accessioned2023-07-06T11:52:31Z
dc.date.available2023-07-06T11:52:31Z
dc.date.issued2022-10-01
dc.description.abstractDermatophytes are pathogenic fungi, comprising the major cause of superficial fungal infections called dermatophytes. Although they infect keratinized tissues such as skin, nail, and hair, invasive serious infections may occur in immunocompromised patients. However, current antifungal drugs show considerable drawbacks, such as toxicity and multiple drug resistance, compelling and directing researches for new antidermatophyte agents. Herein, a series of hydroxypyrone bearing compounds inspired from the natural metabolite kojic acid was reported. Their antidermatophytic effects of the compounds against Microsporum gypseum, Trichophyton mentagrophytes var. erinaceid, and Epidermophyton floccosum were evaluated. The cytotoxicity of the compounds on healthy (MRC-5) and carcinogenic (He-La) cell lines was also investigated, and their cytopathogenic effects were expressed as maximum non-toxic concentrations. According to the activity studies, compounds 10 and 22 were found as the most promising antidermatophytic agents (MIC: 2 mu g/ml), exhibiting comparable effect with that of griseofulvin (MIC: 0.5-1 mu g/ml) and terbinafine (MIC: 0.125-0.5 mu g/ml) which are the most widely used agents for treating mycoses caused by dermatophytes. Molecular docking analysis of the most active compounds, compound 10 and compound 22, with homology model of beta-tubulin protein was carried out to investigate the possible binding conformation of the compounds in the targeted macromolecule.
dc.identifier.citationKarakaya G., Ozdemir A., Ture A., ÖZÇELİK B., Aytemir M., "Synthesis and molecular modeling of some novel hydroxypyrone derivatives as antidermatophytic agents", JOURNAL OF HETEROCYCLIC CHEMISTRY, cilt.59, sa.10, ss.1801-1812, 2022
dc.identifier.doi10.1002/jhet.4520
dc.identifier.endpage1812
dc.identifier.issn0022-152X
dc.identifier.issue10
dc.identifier.startpage1801
dc.identifier.urihttps://hdl.handle.net/11424/290873
dc.identifier.volume59
dc.language.isoeng
dc.relation.ispartofJOURNAL OF HETEROCYCLIC CHEMISTRY
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectKimya
dc.subjectBiyokimya
dc.subjectBiyoinorganik Kimya
dc.subjectTemel Bilimler
dc.subjectChemistry
dc.subjectBiochemistry
dc.subjectBioinorganic Chemistry
dc.subjectNatural Sciences
dc.subjectKİMYA, ORGANİK
dc.subjectTemel Bilimler (SCI)
dc.subjectCHEMISTRY, ORGANIC
dc.subjectCHEMISTRY
dc.subjectNatural Sciences (SCI)
dc.subjectKimya (çeşitli)
dc.subjectOrganik Kimya
dc.subjectGenel Kimya
dc.subjectFizik Bilimleri
dc.subjectChemistry (miscellaneous)
dc.subjectOrganic Chemistry
dc.subjectGeneral Chemistry
dc.subjectPhysical Sciences
dc.titleSynthesis and molecular modeling of some novel hydroxypyrone derivatives as antidermatophytic agents
dc.typearticle
dspace.entity.typePublication
local.avesis.id6e224003-f619-4776-96ad-2f75b0f1d897
local.indexed.atWOS
local.indexed.atSCOPUS
relation.isAuthorOfPublication515da16e-3e07-453b-bfbb-c60fbd768648
relation.isAuthorOfPublication.latestForDiscovery515da16e-3e07-453b-bfbb-c60fbd768648

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