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Synthesis and Anticancer and Antimicrobial Evaluation of Novel Ether-linked Derivatives of Ornidazole

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dc.contributor.authorKÜÇÜKGÜZEL, İLKAY
dc.contributor.authorsSenkardes, Sevil; Kulabas, Necta; Bingol Ozakpinar, Ozlem; Kalayci, Sadik; Sahin, Fikrettin; Kucukguzel, Ilkay; Kucukguzel, S. Guniz
dc.date.accessioned2022-03-14T10:53:27Z
dc.date.available2022-03-14T10:53:27Z
dc.date.issued2020-02-01
dc.description.abstractObjectives: Some novel 1-(2-methyl-5-nitro-1H-imidazol-1-yl)-3-(substituted phenoxy)propan-2-ol derivatives (3a-g) were designed and synthesized. Materials and Methods: Compounds 3a-g were obtained by refluxing ornidazole (1) with the corresponding phenolic compounds (2a-g) in the presence of anhydrous K2CO3 in acetonitrile. Results: Following the structure elucidation, the in vitro antimicrobial activity and cytotoxic effects of compounds 3a-g on K562 leukemia and NIH/3T3 mouse embryonic fibroblast cells were measured. As a part of this study, the compliance of the compounds with the drug-likeness properties was evaluated. The physico-chemical parameters (log P, TPSA, nrotb, number of hydrogen bond donors and acceptors, logS) were calculated using the software OSIRIS. Conclusion: All the synthesized compounds except 3a showed significant activity (MIC=4-16 mu g mL(-)(1)) against the bacterial strain Bacillus subtilis as compared to the standard drug, whereas antileukemic activities were rather limited. Furthermore, all the compounds were nontoxic and the selectivity index outcome indicated that the antileukemic and antimicrobial effects of the compounds were selective with good estimated oral bioavailability and drug-likeness scores.
dc.identifier.doi10.4274/tjps.galenos.2018.59389
dc.identifier.issn1304-530X
dc.identifier.pubmed32454765
dc.identifier.urihttps://hdl.handle.net/11424/245325
dc.identifier.wosWOS:000518401500012
dc.language.isoeng
dc.publisherTURKISH PHARMACISTS ASSOC
dc.relation.ispartofTURKISH JOURNAL OF PHARMACEUTICAL SCIENCES
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectImidazole
dc.subjectether linked
dc.subjectornidazole
dc.subjectantimicrobial activity
dc.subjectcytotoxicity
dc.subjectBIOLOGICAL EVALUATION
dc.subjectDRUG DISCOVERY
dc.subjectANTIBACTERIAL
dc.subjectDESIGN
dc.subjectIMIDAZOLES
dc.titleSynthesis and Anticancer and Antimicrobial Evaluation of Novel Ether-linked Derivatives of Ornidazole
dc.typearticle
dspace.entity.typePublication
local.avesis.id01672b24-5c18-49f3-98b0-c7b1cc99c118
local.import.packageSS16
local.indexed.atWOS
local.indexed.atSCOPUS
local.indexed.atPUBMED
local.indexed.atTRDIZIN
local.journal.numberofpages13
oaire.citation.endPage93
oaire.citation.issue1
oaire.citation.startPage81
oaire.citation.titleTURKISH JOURNAL OF PHARMACEUTICAL SCIENCES
oaire.citation.volume17
relation.isAuthorOfPublication39266c2c-11fd-48a6-8455-d3ea2f2956ed
relation.isAuthorOfPublication.latestForDiscovery39266c2c-11fd-48a6-8455-d3ea2f2956ed

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