DESIGN, SYNTHESIS, MOLECULAR DOCKING, AND
ANTIBACTERIAL ACTIVITY EVALUATION OF SOME NOVEL
NORFLOXACIN ANALOGUES
SMARANDA ONIGA 1#, MARIANA PALAGE 1, CĂTĂLIN ARANICIU 1, GABRIEL MARC 2#, OVIDIU ONIGA 2*, LAURIAN VLASE 3, VIOREL PRISĂCARI 4#, VLADIMIR VALICA 5,6, SERGHEI CURLAT 7, LIVIA UNCU 5,6
1Department of Therapeutic Chemistry, Faculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy,
Cluj-Napoca, Romania
2Department of Pharmaceutical Chemistry, Faculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy,
Cluj-Napoca, Romania
3Department of Pharmaceutical Technology and Biopharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy,
Cluj-Napoca, Romania
4Epidemiology, Faculty of Medicine, “Nicolae Testemițanu" State University of Medicine and Pharmacy, Chișinău, Republic
of Moldova
5Pharmaceutical Chemistry and Toxicology, Faculty of Pharmacy, “Nicolae Testemițanu" State University of Medicine and
Pharmacy, Chișinău, Republic of Moldova
6Scientific Centre of Drug Research, “Nicolae Testemițanu" State University of Medicine and Pharmacy, Chișinău, Republic
of Moldova
7Biochemistry and Clinical Biochemistry, Faculty of Medicine, “Nicolae Testemițanu" State University of Medicine and
Pharmacy, Chișinău, Republic of Moldova
*corresponding author: ooniga@umfcluj.ro
#Authors with equal contribution
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Abstract:
A novel series of 7 or 3-substituted norfloxacin derivatives were synthesized and characterized by 1H NMR, MS and elemental
analysis techniques. All the synthesized compounds were evaluated for antimicrobial activity against both Gram-positive and
Gram-negative bacteria and the MIC and MBC values were calculated by the broth dilution method. To understand the
influence of the different type of substituents on the pharmacokinetic properties and the interaction with the target enzyme of
fluoroquinolones (DNA gyrase), we performed a molecular docking study, and we calculated the ADMET properties.
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