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Novel fluoroquinolones containing 2-arylamino-2-oxoethyl fragment: Design, synthesis, evaluation of antibacterial and antituberculosis activities and molecular modeling studies

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dc.contributor.authorTÜRE, ASLI
dc.contributor.authorsKulabas, Necla; Ture, Asli; Bozdeveci, Arif; Krishna, Vagolu Siva; Karaoglu, Sengul Alpay; Sriram, Dharmarajan; Kucukguzel, Ilkay
dc.date.accessioned2022-03-23T09:35:11Z
dc.date.available2022-03-23T09:35:11Z
dc.date.issued2022
dc.description.abstractNovel substituted fluoroquinolone derivatives, compounds 6-20 were designed, synthesized, and evaluated for antituberculosis and antibacterial activity. Antibacterial activities of the compounds were determined and compound 14 was found to be the most potent antimicrobial agent owing to minimal inhibitory concentration (MIC) value of <1.16 mu g/mu l for all tested bacteria. Further, compounds were tested in vitro for their antimycobacterial activity against Mycobacterium tuberculosis H37Rv. Most of the compounds showed antimycobacterial effects with 1.56-25.00 mu g/ml MIC values. Compounds 14 and 18 were found to be the most active derivatives due to their MIC at 1.56 mu g/ml. Selected compounds 11, 14, 17, and 18 were tested for M. tuberculosis DNA supercoiling assay and they had IC50 values within a range of 6.35-15 mu M. Mechanism of binding to DNA gyrase enzymes was evaluated using in silico molecular modeling studies and it was shown that compounds 6-20 adopt a similar binding mode as already known for fluoroquinolone drugs.
dc.identifier.doi10.1002/jhet.4430
dc.identifier.eissn1943-5193
dc.identifier.issn0022-152X
dc.identifier.urihttps://hdl.handle.net/11424/254625
dc.identifier.wosWOS:000737096900001
dc.language.isoeng
dc.publisherWILEY
dc.relation.ispartofJOURNAL OF HETEROCYCLIC CHEMISTRY
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectMICROWAVE-ASSISTED SYNTHESIS
dc.subjectMYCOBACTERIUM-TUBERCULOSIS
dc.subjectBIOLOGICAL EVALUATION
dc.subjectANTIMYCOBACTERIAL EVALUATION
dc.subjectDERIVATIVES
dc.subjectCIPROFLOXACIN
dc.subjectMOXIFLOXACIN
dc.subjectANTICANCER
dc.subjectGATIFLOXACIN
dc.subjectINHIBITION
dc.titleNovel fluoroquinolones containing 2-arylamino-2-oxoethyl fragment: Design, synthesis, evaluation of antibacterial and antituberculosis activities and molecular modeling studies
dc.typearticle
dspace.entity.typePublication
local.avesis.id4b2e4c90-c919-4492-8d4a-b60d6d7412c6
local.import.packageSS26
local.indexed.atWOS
local.journal.numberofpages18
oaire.citation.titleJOURNAL OF HETEROCYCLIC CHEMISTRY
relation.isAuthorOfPublication515da16e-3e07-453b-bfbb-c60fbd768648
relation.isAuthorOfPublication.latestForDiscovery515da16e-3e07-453b-bfbb-c60fbd768648

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