Romanian Society of Pharmaceutical Sciences
 

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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

1.Department of Therapeutic Chemistry, Faculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, Cluj-Napoca, Romania
2.Department of Pharmaceutical Chemistry, Faculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, Cluj-Napoca, Romania
3.Department of Pharmaceutical Technology and Biopharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, Cluj-Napoca, Romania
4.Epidemiology, Faculty of Medicine, “Nicolae Testemițanu" State University of Medicine and Pharmacy, Chișinău, Republic of Moldova
5.Pharmaceutical Chemistry and Toxicology, Faculty of Pharmacy, “Nicolae Testemițanu" State University of Medicine and Pharmacy, Chișinău, Republic of Moldova
6.Scientific Centre of Drug Research, “Nicolae Testemițanu" State University of Medicine and Pharmacy, Chișinău, Republic of Moldova
7.Biochemistry and Clinical Biochemistry, Faculty of Medicine, “Nicolae Testemițanu" State University of Medicine and Pharmacy, Chișinău, Republic of Moldova

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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.