Design, Synthesis and Biological Evaluation of New Piperazin-4-yl-(acetyl-thiazolidine-2,4-dione) Norfloxacin Analogues as Antimicrobial Agents.

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ID: 78131
2019
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Abstract
In an effort to improve the antimicrobial activity of norfloxacin, a series of hybrid norfloxacin-thiazolidinedione molecules were synthesized and screened for their direct antimicrobial activity and their anti-biofilm properties. The new hybrids were intended to have a new binding mode to DNA gyrase, that will allow for a more potent antibacterial effect, and for activity against current quinolone-resistant bacterial strains. Moreover, the thiazolidinedione moiety aimed to include additional anti-pathogenicity by preventing biofilm formation. The resulting compounds showed promising direct activity against Gram-negative strains, and anti-biofilm activity against Gram-positive strains. Docking studies and ADMET were also used in order to explain the biological properties and revealed some potential advantages over the parent molecule norfloxacin.
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marc2019designmolecules Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Marc, Gabriel;Araniciu, Cătălin;Oniga, Smaranda Dafina;Vlase, Laurian;Pîrnău, Adrian;Nadăș, George Cosmin;Novac, Cristiana Ștefania;Matei, Ioana Adriana;Chifiriuc, Mariana Carmen;Măruțescu, Luminița;Oniga, Ovidiu;
Journal molecules
Year 2019
DOI
E3959
URL
Keywords
antibiotic resistance fluoroquinolones thiazolidinedione dna gyrase anti-bacterial anti-biofilm norfloxacin

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