Статья

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

Gabriel MarcFaculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, 8 Victor Babes Street, 400012 Cluj-Napoca, RomaniaCătălin AraniciuFaculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, 8 Victor Babes Street, 400012 Cluj-Napoca, RomaniaSmaranda OnigaFaculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, 8 Victor Babes Street, 400012 Cluj-Napoca, RomaniaLaurian VlaseFaculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, 8 Victor Babes Street, 400012 Cluj-Napoca, RomaniaAdrian Pı̂rnăuNational Institute for Research and Development of Isotopic and Molecular Technologies, 67-103 Donath Street, 400293 Cluj-Napoca, RomaniaG. NadăşDepartment of Microbiology, Faculty of Veterinary Medicine, University of Agricultural Sciences and Veterinary Medicine, 3-5 Mănăștur Street, 400372 Cluj-Napoca, RomaniaCristiana Ștefania NovacDepartment of Microbiology, Faculty of Veterinary Medicine, University of Agricultural Sciences and Veterinary Medicine, 3-5 Mănăștur Street, 400372 Cluj-Napoca, RomaniaIoana Adriana MateiDepartment of Microbiology, Faculty of Veterinary Medicine, University of Agricultural Sciences and Veterinary Medicine, 3-5 Mănăștur Street, 400372 Cluj-Napoca, RomaniaMariana Carmen ChifiriucDepartment of Microbiology, Faculty of Biology, University of Bucharest, 1-3 Portocalelor Street, 60101 Bucharest, RomaniaLuminița MăruțescuDepartment of Microbiology, Faculty of Biology, University of Bucharest, 1-3 Portocalelor Street, 60101 Bucharest, RomaniaOvidiu OnigaFaculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, 8 Victor Babes Street, 400012 Cluj-Napoca, Romania

2019en

ABI

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.

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Идентификаторы

DOI: 10.3390/molecules24213959

Цитирования и источники

Цитирований: 2Использованных источников: 0

Показатели — AkademScholar