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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.authorALPAY KARAOĞLU, ŞENGÜL
dc.contributor.authorKULABAŞ, NECLA
dc.contributor.authorDingis, SERAP İPEK
dc.contributor.authorBirgul, Kaan
dc.contributor.authorBozdeveci, Arif
dc.contributor.authorKrishna, Vagolu Siva
dc.contributor.authorSriram, Dharmarajan
dc.contributor.authorKÜÇÜKGÜZEL, İLKAY
dc.contributor.institutionauthorDİNGİŞ BİRGÜL, SERAP İPEK
dc.date.accessioned2021-09-21T20:59:20Z
dc.date.available2021-09-21T20:59:20Z
dc.date.issued2019-07-01T00:00:00Z
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.citationTÜRE A., KULABAŞ N., Dingis S. İ. , Birgul K., Bozdeveci A., ALPAY KARAOĞLU Ş., Krishna V. S. , Sriram D., KÜÇÜKGÜZEL İ., -Design, synthesis and molecular modeling studies on novel moxifloxacin derivatives as potential antibacterial and antituberculosis agents-, BIOORGANIC CHEMISTRY, cilt.88, 2019
dc.identifier.doi10.1016/j.bioorg.2019.102965
dc.identifier.scopus85065416523
dc.identifier.urihttp://hdl.handle.net/20.500.12645/29490
dc.identifier.wosWOS:000475378400058
dc.titleDesign, synthesis and molecular modeling studies on novel moxifloxacin derivatives as potential antibacterial and antituberculosis agents
dc.typeArticle
dspace.entity.typePublication
local.avesis.ide56f6a42-9321-4f65-a1e1-5df1cea61f92
local.publication.goal03 - Sağlık ve Kaliteli Yaşam
local.publication.isinternational1
relation.isAuthorOfPublication3e5ffe11-c413-4a43-91ed-06e0978e0b21
relation.isAuthorOfPublication.latestForDiscovery3e5ffe11-c413-4a43-91ed-06e0978e0b21
relation.isGoalOfPublication9c198c48-b603-4e2f-8366-04edcfc1224c
relation.isGoalOfPublication.latestForDiscovery9c198c48-b603-4e2f-8366-04edcfc1224c
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