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

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.

SUBMITTER: Marc G 

PROVIDER: S-EPMC6864599 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature

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

Marc Gabriel G   Araniciu Cătălin C   Oniga Smaranda Dafina SD   Vlase Laurian L   Pîrnău Adrian A   Nadăș George Cosmin GC   Novac Cristiana Ștefania CȘ   Matei Ioana Adriana IA   Chifiriuc Mariana Carmen MC   Măruțescu Luminița L   Oniga Ovidiu O  

Molecules (Basel, Switzerland) 20191031 21

<b>&nbsp;</b>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  ...[more]

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