Molecules (Basel, Switzerland) · 2019
Design, Synthesis and Biological Evaluation of New Piperazin-4-yl-(acetyl-thiazolidine-2,4-dione) Norfloxacin Analogues as Antimicrobial Agents.
СтатьяНазвание и аннотация: Перевод пока не подготовлен
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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
Аннотация
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.