Unknown

Dataset Information

0

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

altmetric image

Publications

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]

Similar Datasets

| S-EPMC5026645 | biostudies-literature
| S-EPMC4158516 | biostudies-literature
| S-EPMC8741387 | biostudies-literature
| S-EPMC10975047 | biostudies-literature
| S-EPMC6154471 | biostudies-literature
| S-EPMC6010082 | biostudies-literature
| S-EPMC3254425 | biostudies-literature
| S-EPMC3998427 | biostudies-literature
| S-EPMC2979635 | biostudies-literature
| S-EPMC3100059 | biostudies-literature