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Synthesis, and prediction of molecular properties and antimicrobial activity of some acylhydrazones derived from N-(arylsulfonyl)methionine

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dc.contributor.authorTATAR, ESRA
dc.contributor.authorsTatar, Esra; Senkardes, Sevil; Sellitepe, Hasan Erdinc; Kucukguzel, Sukriye Guniz; Karaoglu, Sengul Alpay; Bozdeveci, Arif; De Clercq, Erik; Pannecouque, Christophe; Ben Hadda, Taibi; Kucukguzel, Ilkay
dc.date.accessioned2022-04-25T00:11:04Z
dc.date.available2022-04-25T00:11:04Z
dc.date.issued2016
dc.description.abstractA series of 38 new acylhydrazones [3-40], derived from (2S)-4-(methylsulfanyl)-2-[[(4-methylphenyl)sulfonyl] amino]butanoic acid hydrazide [2], were synthesized and evaluated for their anti-HIV and antimicrobial activity with the further aim to develop acylhydrazones carrying an amino acid side chain. All tested compounds possess stronger activity against gram (+) bacteria. Compound 23 was found active against methicillin-resistant Staphylococcus aureus (MRSA) with a MIC value of 3.9 mu g/mL. The MIC value of compound 30 against Enterococcus faecalis, Listeria monocytogenes, and Bacillus cereus was 8 mu g/mL. A computational study for prediction of ADME and drug-like properties (solubility, drug-likeness, and drug score) as well as potential toxicity profiles of compounds 2-40 was performed using the Molinspiration online property calculation toolkit and Osiris Property Explorer. As most of our compounds meet Lipinski's rule of five, they promise good solubility and permeability. According to Osiris calculations, the majority of our compounds are supposed to be nonmutagenic and nonirritating.
dc.identifier.doi10.3906/kim-1509-21
dc.identifier.issn1300-0527
dc.identifier.urihttps://hdl.handle.net/11424/263832
dc.identifier.wosWOS:000376305300013
dc.languageeng
dc.publisherSCIENTIFIC TECHNICAL RESEARCH COUNCIL TURKEY-TUBITAK
dc.relation.ispartofTURKISH JOURNAL OF CHEMISTRY
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectAcylhydrazones
dc.subjectantimicrobial activity
dc.subjectL-methionine
dc.subjectmicrowave-assisted synthesis
dc.subjectMRSA
dc.subjectHIV-1 REVERSE-TRANSCRIPTASE
dc.subjectPROTEIN SYNTHASE III
dc.subjectRIBONUCLEASE-H
dc.subjectHYDRAZIDE DERIVATIVES
dc.subjectBIOLOGICAL-ACTIVITIES
dc.subjectANTIVIRAL EVALUATION
dc.subjectANTIFUNGAL ACTIVITY
dc.subjectCOLORIMETRIC ASSAY
dc.subjectN-ACYLHYDRAZONES
dc.subjectANTI-HIV
dc.titleSynthesis, and prediction of molecular properties and antimicrobial activity of some acylhydrazones derived from N-(arylsulfonyl)methionine
dc.typearticle
dspace.entity.typePublication
local.avesis.id8b88a388-c713-4334-a8c5-0a5cf8282b5a
local.import.packageSS39
local.indexed.atWOS
local.journal.numberofpages25
local.journal.quartileQ3
oaire.citation.endPage534
oaire.citation.issue3
oaire.citation.startPage510
oaire.citation.titleTURKISH JOURNAL OF CHEMISTRY
oaire.citation.volume40
relation.isAuthorOfPublicatione2c939bf-1387-4174-802c-e714419b20af
relation.isAuthorOfPublication.latestForDiscoverye2c939bf-1387-4174-802c-e714419b20af

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