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Synthesis, antimicrobial properties and in silico studies of aryloxyacetic acid derivatives with hydrazone or thiazolidine-4-one scaffold

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dc.contributor.authorŞENKARDEŞ, SEVİL
dc.contributor.authorsŞENKARDEŞ S., KART D., Bebek B., GÜNDÜZ M. G. , Kucukguzel S. G.
dc.contributor.departmentDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Maltepe, Marmara University
dc.date.accessioned2022-09-27T06:33:07Z
dc.date.available2022-09-27T06:33:07Z
dc.date.issued2022-09-01
dc.description.abstractIn this work, twenty hydrazide-hydrazone and 4-thiazolidinone derivatives were synthesized starting from m-cresol. Antimicrobial evaluation was carried out by microdilution method against Enterococcus faecalis and Staphylococcus aureus as Gram-positive bacteria and Escherichia coli and Pseudomonas aeruginosa as Gram-negative bacteria, and three pathogenic fungi Candida albicans, Candida parapsilosis and Candida krusei. Some compounds possessed considerable antimicrobial properties against the tested microorganisms, particularly against E. coli. 4-Thiazolidinones containing 3-methoxyphenyl and 3,5-dichlorophenyl moieties (4h and 4i) were found to be the most active derivatives with MICs of 2 mu g/mL against E. coli. N\"-[(3,5-dichlorophenyl)methylidene]-2-(3-methylphenoxy)acetohydrazide (3i) also displayed antifungal activity against Candida krusei that was comparable to fluconazole. Calculated drug-likeness and ADMET parameters of the most active compounds confirmed their potential as antimicrobial drug candidates. Molecular docking investigations were carried out in the thiamine diphosphate-binding site of pyruvate dehydrogenase multienzyme complex E1 component (PDHc-E1) to clarify the potential antibacterial mechanism against E. coli. The results showed the potential and importance of developing new hydrazones and 4-thiazolidinones that would be effective against microbial strains. Communicated by Ramaswamy H. Sarma
dc.identifier.citationŞENKARDEŞ S., KART D., Bebek B., GÜNDÜZ M. G. , Kucukguzel S. G. , "Synthesis, antimicrobial properties and in silico studies of aryloxyacetic acid derivatives with hydrazone or thiazolidine-4-one scaffold", JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS, 2022
dc.identifier.doi10.1080/07391102.2022.2121761
dc.identifier.issn0739-1102
dc.identifier.urihttps://hdl.handle.net/11424/281777
dc.language.isoeng
dc.relation.ispartofJOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectTıp
dc.subjectYaşam Bilimleri
dc.subjectMoleküler Biyoloji ve Genetik
dc.subjectSitogenetik
dc.subjectSağlık Bilimleri
dc.subjectTemel Tıp Bilimleri
dc.subjectBiyofizik
dc.subjectBiyokimya
dc.subjectTemel Bilimler
dc.subjectMedicine
dc.subjectLife Sciences
dc.subjectMolecular Biology and Genetics
dc.subjectCytogenetic
dc.subjectHealth Sciences
dc.subjectFundamental Medical Sciences
dc.subjectBiophysics
dc.subjectBiochemistry
dc.subjectNatural Sciences
dc.subjectBİYOKİMYA VE MOLEKÜLER BİYOLOJİ
dc.subjectYaşam Bilimleri (LIFE)
dc.subjectBİYOFİZİK
dc.subjectBiyoloji ve Biyokimya
dc.subjectBIOCHEMISTRY & MOLECULAR BIOLOGY
dc.subjectMOLECULAR BIOLOGY & GENETICS
dc.subjectLife Sciences (LIFE)
dc.subjectBIOPHYSICS
dc.subjectBIOLOGY & BIOCHEMISTRY
dc.subjectİlaç Keşfi
dc.subjectBiyokimya (tıbbi)
dc.subjectYapısal Biyoloji
dc.subjectMoleküler Biyoloji
dc.subjectKlinik Biyokimya
dc.subjectKanser Araştırmaları
dc.subjectYaşlanma
dc.subjectBiyokimya, Genetik ve Moleküler Biyoloji (çeşitli)
dc.subjectGenel Biyokimya, Genetik ve Moleküler Biyoloji
dc.subjectDrug Discovery
dc.subjectBiochemistry (medical)
dc.subjectStructural Biology
dc.subjectMolecular Biology
dc.subjectClinical Biochemistry
dc.subjectCancer Research
dc.subjectAging
dc.subjectBiochemistry, Genetics and Molecular Biology (miscellaneous)
dc.subjectGeneral Biochemistry, Genetics and Molecular Biology
dc.titleSynthesis, antimicrobial properties and in silico studies of aryloxyacetic acid derivatives with hydrazone or thiazolidine-4-one scaffold
dc.typearticle
dspace.entity.typePublication
local.avesis.idd15035c4-5b11-4cc5-a698-e914f1a96e1c
local.indexed.atPUBMED
relation.isAuthorOfPublicationf046c84e-6096-4def-ac1f-8be5d9ef3a52
relation.isAuthorOfPublication.latestForDiscoveryf046c84e-6096-4def-ac1f-8be5d9ef3a52

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