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Design, synthesis and molecular modeling studies on novel moxifloxacin derivatives as potential antibacterial and antituberculosis agents

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dc.contributor.authorTÜRE, ASLI
dc.contributor.authorsTure, Asli; Kulabas, Necla; Dingis, Serap Ipek; Birgul, Kaan; Bozdeveci, Arif; Karaoglu, Sengul Alpay; Krishna, Vagolu Siva; Sriram, Dharmarajan; Kucukguzel, Ilkay
dc.date.accessioned2022-03-12T16:24:24Z
dc.date.available2022-03-12T16:24:24Z
dc.date.issued2019
dc.description.abstractTwenty-one novel alkyl/acyl/sulfonyl substituted fluoroquinolone derivatives were designed, synthesized and evaluated for their anti-tuberculosis and antibacterial activity. The targeted compounds were synthesized by the introduction of alkyl, acyl or sulfonyl moieties to the basic secondary amine moiety of moxifloxacin. Structures of the compounds were enlightened by FT-IR, H-1 NMR, C-13 NMR and HRMS data besides elemental analysis. Compounds were initially tested in vitro for their anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv using microplate alamar blue assay. Minimal inhibitory concentration (MIC) values of all compounds were found between > 25.00-0.39 mu g/mL while compounds 1, 2 and 13 revealed an outstanding activity against M. tuberculosis H37Rv with MIC values of 0.39 mu g/mL. Activities of compounds 1-21 against to a number of Gram-positive and Gram-negative bacteria and fast growing mycobacterium strain were also investigated by agar well diffusion and microdilution methods. According to antimicrobial activity results, compound 13 was found the most potent derivative with a IC50 value of < 1.23 mu g/mL against Staphylococcus aureus and clinical strain of methicillin-resistant clinical strain of S. aureus.
dc.identifier.doi10.1016/j.bioorg.2019.102965
dc.identifier.eissn1090-2120
dc.identifier.issn0045-2068
dc.identifier.pubmed31085371
dc.identifier.urihttps://hdl.handle.net/11424/226331
dc.identifier.wosWOS:000475378400058
dc.language.isoeng
dc.publisherACADEMIC PRESS INC ELSEVIER SCIENCE
dc.relation.ispartofBIOORGANIC CHEMISTRY
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectFluoroquinolones
dc.subjectMoxifloxacin
dc.subjectAntibacterial activity
dc.subjectAnti-tuberculosis activity
dc.subjectDNA supercoiling assay
dc.subjectMolecular docking
dc.subjectResistant strains
dc.subjectBIOLOGICAL EVALUATION
dc.subjectCIPROFLOXACIN DERIVATIVES
dc.subjectTOPOISOMERASE-I
dc.subjectDNA GYRASE
dc.subjectHYBRIDS
dc.subjectFLUOROQUINOLONES
dc.subjectANTICANCER
dc.subjectINHIBITORS
dc.subjectQUINOLONE
dc.subjectCOMPLEXES
dc.titleDesign, synthesis and molecular modeling studies on novel moxifloxacin derivatives as potential antibacterial and antituberculosis agents
dc.typeconferenceObject
dspace.entity.typePublication
local.avesis.ide56f6a42-9321-4f65-a1e1-5df1cea61f92
local.conference.dateAUG 27-31, 2017
local.conference.locationVienna, AUSTRIA
local.conference.sponsorEFMC
local.conference.title7th EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry
local.import.packageSS15
local.indexed.atWOS
local.indexed.atSCOPUS
local.indexed.atPUBMED
local.journal.articlenumber102965
local.journal.numberofpages11
local.journal.quartileQ1
oaire.citation.titleBIOORGANIC CHEMISTRY
oaire.citation.volume88
relation.isAuthorOfPublication515da16e-3e07-453b-bfbb-c60fbd768648
relation.isAuthorOfPublication.latestForDiscovery515da16e-3e07-453b-bfbb-c60fbd768648

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