NEW SULFONAMIDO-BENZOXAZOLE DERIVATIVES AS ANTIMICROBIAL AGENTS: DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION

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dc.authorscopusid57215604118
dc.authorscopusid58881241200
dc.authorscopusid57217235268
dc.authorscopusid57479331400
dc.authorscopusid6602689055
dc.contributor.authorErol M.
dc.contributor.authorAcar-Halici C.
dc.contributor.authorKuyucuklu G.
dc.contributor.authorSalan A.S.
dc.contributor.authorTemiz Arpaci O.
dc.date.accessioned2024-06-12T10:25:58Z
dc.date.available2024-06-12T10:25:58Z
dc.date.issued2024
dc.description.abstractObjective: Many investigations are conducted in the battle against infectious diseases in order to develop new drug-active ingredient candidate compounds and to identify leading compounds. The goal of this study was to synthesis a total of seven compounds, six of which are novel, with the general structure 2-(4-tert-butylphenyl)-5-(4-substitutedphenylsulfonamido)benzoxazole, to elucidate their structures, and to test their antimicrobial activities using the microdilution method. Material and Method: The synthesis of the compounds was carried out in two stages. In the first stage, under PPA catalyst 2,4-diaminophenol and 4-tert-butylbenzoic acid were refluxed, and target compounds were produced in the second step by reacting 4-substitutedbenzenesulfonyl chloride with 5-Amino-2-(4-tert-butylphenyl)benzoxazole. The compounds' antimicrobial activity was determined by using Enterococcus faecalis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, and drug-resistant strains of these microorganisms in vitro antimicrobial activity studies. Furthermore, estimated ADME profiles were calculated using the SwissADME online software. Result and Discussion: The structures of the synthesized compounds were elucidated using 1H-NMR, 13C-NMR and Mass spectroscopy, and also their melting points were determined. The antimicrobial activities of the compounds ranged from 64 µg/ml to >512 µg/ml and were weaker than the reference drugs. The best antimicrobial activity was reported against an isolate of E. faecalis, with all compounds having MIC values of 64 µg/ml. The fact that six of the seven synthesized compounds are novel and that their antimicrobial activity will be tested for the first time will make a significant contribution to studies to develop new or alternative antimicrobial agents. © 2024 University of Ankara. All rights reserved.en_US
dc.identifier.doi10.33483/jfpau.1341483
dc.identifier.issn2564-6524
dc.identifier.issue1en_US
dc.identifier.scopus2-s2.0-85184778891en_US
dc.identifier.scopusqualityN/Aen_US
dc.identifier.trdizinid1222548en_US
dc.identifier.urihttps://doi.org/10.33483/jfpau.1341483
dc.identifier.urihttps://search.trdizin.gov.tr/yayin/detay/1222548
dc.identifier.urihttps://hdl.handle.net/20.500.14551/16609
dc.identifier.volume48en_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakTR-Dizinen_US
dc.language.isoenen_US
dc.publisherUniversity of Ankaraen_US
dc.relation.ispartofAnkara Universitesi Eczacilik Fakultesi Dergisien_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectAdme; Antimicrobial Activity; Benzoxazole; Sulfonamideen_US
dc.subject2 (4 Tert Butylphenyl) 5 (4 Chlorophenylsulfonamido)Benzoxazole; 2 (4 Tert Butylphenyl) 5 (4 Fluorophenylsulfonamido)Benzoxazole; 2 (4 Tert Butylphenyl) 5 (4 Methoxyphenylsulfonamido)Benzoxazole; 2 (4 Tert Butylphenyl) 5 (4 Nitrophenylsulfonamido)Benzoxazole; 2 (4 Tert Butylphenyl) 5 (Phenylsulfonamido)Benzoxazole; 2 (4 Tert-Butylphenyl) 5 (4 Bromophenylsulfonamido)Benzoxazole; 2 (4 Tert-Butylphenyl) 5 (4 Methylphenylsulfonamido)Benzoxazole; Amphotericin B; Ampicillin; Antiinfective Agent; Benzoxazole Derivative; Ciprofloxacin; Gentamicin; Meropenem; Sulfonamide; Unclassified Drug; Vancomycin; Antibiotic Resistance; Antimicrobial Activity; Article; Bacterial Strain; Bacterium Isolate; Candida Albicans; Carbon Nuclear Magnetic Resonance; Controlled Study; Drug Design; Drug Screening; Drug Structure; Drug Synthesis; Enterococcus Faecalis; Escherichia Coli; In Vitro Study; Lipophilicity; Mass Spectrometry; Melting Point; Minimum Inhibitory Concentration; Molecular Weight; Nonhuman; Physical Chemistry; Proton Nuclear Magnetic Resonance; Pseudomonas Aeruginosa; Staphylococcus Aureus; Structure Analysis; Substitution Reaction; Water Solubilityen_US
dc.titleNEW SULFONAMIDO-BENZOXAZOLE DERIVATIVES AS ANTIMICROBIAL AGENTS: DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATIONen_US
dc.title.alternativeANTİMİKROBİYAL AJAN OLARAK YENİ SÜLFONAMİDO-BENZOKSAZOL TÜREVLERİ: TASARIM, SENTEZ VE BİYOLOJİK DEĞERLENDİRMEen_US
dc.typeArticleen_US

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