Design, synthesis and docking studies of quinoline-oxazolidinone hybrid molecules and their antitubercular properties

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dc.contributor.authorThomas, K.D.
dc.contributor.authorVasudeva Adhikari, A.V.
dc.contributor.authorChowdhury, I.H.
dc.contributor.authorSandeep, T.
dc.contributor.authorMahmood, R.
dc.contributor.authorBhattacharya, B.
dc.contributor.authorSumesh, E.
dc.date.accessioned2026-02-05T09:35:38Z
dc.date.issued2011
dc.description.abstractNew series of quinoline-oxazolidinone hybrid molecules were synthesized based on the preliminary docking studies. All the newly synthesized compounds were characterized by spectral analyses. The newly synthesized compounds were screened for their antimycobacterial properties based on the promising preliminary antibacterial screening results. Amongst tested compounds, compounds 8a, 8j and 13a were active at 0.65 ?g/mL against Mycobacterium tuberculosis H <inf>37</inf>Rv strain. The mode of action of these active compounds was carried out by docking of receptor enoyl-ACP reductase with newly synthesized candidate ligands 8a, 8j and 13a. These compounds exhibited well established bonds with one or more amino acids in the receptor active pocket. From the docking studies, compound 8j was considered to be the best inhibitor. © 2011 Elsevier Masson SAS. All rights reserved.
dc.identifier.citationEuropean Journal of Medicinal Chemistry, 2011, 46, 10, pp. 4834-4845
dc.identifier.issn2235234
dc.identifier.urihttps://doi.org/10.1016/j.ejmech.2011.07.049
dc.identifier.urihttps://idr.nitk.ac.in/handle/123456789/27176
dc.subject2 (5 cyclopentylaminomethyl 2 oxo oxazolidin 3 yl) n (6 methoxy 2 methyl quinolin 4 yl)acetamide
dc.subject2 (5 cyclopropylaminomethyl 2 oxo oxazolidin 3 yl) n (6 methoxy 2 methyl quinolin 4 yl)acetamide
dc.subject2 (5 diethylaminomethyl 2 oxo oxazolidin 3 yl) n (6 methoxy 2 methyl quinolin 4 yl)acetamide
dc.subject2 (5 dimethylaminomethyl 2 oxo oxazolidin 3 yl) n (6 methoxy 2 methyl quinolin 4 yl)acetamide
dc.subject2 [5 ((4 acetyl piperazin 1 yl)methyl) 2 oxo oxazolidin 3 yl] n (6 methoxy 2 methyl quinolin 4 yl)acetamide
dc.subject2 [5 ((4 ethyl piperazin 1 yl)methyl) 2 oxo oxazolidin 3 yl] n (6 methoxy 2 methyl quinolin 4 yl)acetamide
dc.subject2 [5 ((4 isopropyl piperazin 1 yl)methyl) 2 oxo oxazolidin 3 yl] n (6 methoxy 2 methyl quinolin 4 yl)acetamide
dc.subject2 [5 ((4 tert butyl piperazin 1 yl)methyl) 2 oxo oxazolidin 3 yl] n (6 methoxy 2 methyl quinolin 4 yl)acetamide
dc.subject2 [5 ((cyclohexyl methyl amino)methyl) 2 oxooxazolidin 3 yl] n (6 methoxy 2 methyl quinolin 4 yl)acetamide
dc.subject2 fluoro n [3 (6 methoxy 2 methyl quinolin 4 yl) 2 oxo oxazolidin 5 ylmethyl]benzamide
dc.subject4 chloro n [3 (6 methoxy 2 methyl quinolin 4 yl) 2 oxo oxazolidin 5 ylmethyl]benzamide
dc.subject4 ethyl n [3 (6 methoxy 2 methyl quinolin 4 yl) 2 oxo oxazolidin 5 ylmethyl]benzamide
dc.subject4 fluoro n [3 (6 methoxy 2 methyl quinolin 4 yl) 2 oxo oxazolidin 5 ylmethyl]benzamide
dc.subject4 methoxy n [3 (6 methoxy 2 methyl quinolin 4 yl) 2 oxo oxazolidin 5 ylmethyl] 2 methylbenzamide
dc.subject4 methoxy n [3 (6 methoxy 2 methyl quinolin 4 yl) 2 oxo oxazolidin 5 ylmethyl]benzamide
dc.subjectn (6 methoxy 2 methyl quinolin 4 yl) 2 (2 oxo 5 piperidin 1 ylmethyl oxazolidin 3 yl)acetamide
dc.subjectn (6 methoxy 2 methyl quinolin 4 yl) 2 (2 oxo 5 pyrrolidin 1 ylmethyl oxazolidin 3 yl)acetamide
dc.subjectn (6 methoxy 2 methyl quinolin 4 yl) 2 (5 morpholin 4 ylmethyl 2 oxo oxazolidin 3 yl)acetamide
dc.subjectn (6 methoxy 2 methyl quinolin 4 yl) 2 [5 ((4 methylpiperazin 1 yl)methyl) 2 oxo oxazolidin 3 yl]acetamide
dc.subjectn (6 methoxy 2 methyl quinolin 4 yl) 2 [5 (4 methylpiperidin 1 ylmethyl) 2 oxo oxazolidin 3 yl]acetamide
dc.subjectn [(3 (6 methoxy 2 methylquinolin 4 yl) 2 oxo 1,3 oxazolidin 5 yl)methyl]acetamide
dc.subjectn [(3 (6 methoxy 2 methylquinolin 4 yl) 2 oxo 1,3 oxazolidin 5 yl)methyl]cyclobutane carboxamide
dc.subjectn [(3 (6 methoxy 2 methylquinolin 4 yl) 2 oxo 1,3 oxazolidin 5 yl)methyl]cyclopropane carboxamide
dc.subjectn [3 (6 methoxy 2 methyl quinolin 4 yl) 2 oxo oxazolidin 5 ylmethyl] 4 methylbenzamide
dc.subjectn [3 (6 methoxy 2 methyl quinolin 4 yl) 2 oxo oxazolidin 5 ylmethyl] 4 trifluoromethylbenzamide
dc.subjectn [3 (6 methoxy 2 methyl quinolin 4 yl) 2 oxo oxazolidin 5 ylmethyl]benzamide
dc.subjectoxazolidinone derivative
dc.subjectquinoline derivative
dc.subjecttuberculostatic agent
dc.subjectunclassified drug
dc.subjectunindexed drug
dc.subjectantibacterial activity
dc.subjectarticle
dc.subjectbacterial strain
dc.subjectcontrolled study
dc.subjectdrug design
dc.subjectdrug receptor binding
dc.subjectdrug screening
dc.subjectdrug synthesis
dc.subjectEscherichia coli
dc.subjectKlebsiella pneumoniae
dc.subjectmolecular docking
dc.subjectMycobacterium fortuitum
dc.subjectMycobacterium smegmatis
dc.subjectMycobacterium tuberculosis
dc.subjectnonhuman
dc.subjectPseudomonas aeruginosa
dc.subjectspectroscopy
dc.subjectStaphylococcus aureus
dc.subjectStreptococcus pyogenes
dc.subjectAnti-Bacterial Agents
dc.subjectAntitubercular Agents
dc.subjectBacteria
dc.subjectCatalytic Domain
dc.subjectDrug Design
dc.subjectEnoyl-(Acyl-Carrier-Protein) Reductase (NADH)
dc.subjectHumans
dc.subjectModels, Molecular
dc.subjectOxazolidinones
dc.subjectProtein Binding
dc.subjectQuinolines
dc.subjectTuberculosis
dc.titleDesign, synthesis and docking studies of quinoline-oxazolidinone hybrid molecules and their antitubercular properties

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