Synthesis and Antibacterial Evaluation of new OfloxacinChalcone derivatives Conjugates as Possible Mutual
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الباحث الأول:
Samer A. Hasan
الباحثين الآخرين:
Noor H. Nasser*, Ahmed K. Hussein*, Abbas H. Abdulsada**, Zainab M. Jasim***, Sarah H. Shaalan****,
and Hawraa K. Musa
المجلة:
journal of pharmaceutical science and research
تاريخ النشر:
None
مختصر البحث:
Objectives:
To synthesize ofloxacin-chalcones conjugates as possible mutual prodrugs of enhanced antibacterial activity and evaluate this activity against
different bacterial strains.
Methods:
Two chalcone derivatives have been synthesized using…
Objectives:
To synthesize ofloxacin-chalcones conjugates as possible mutual prodrugs of enhanced antibacterial activity and evaluate this activity against
different bacterial strains.
Methods:
Two chalcone derivatives have been synthesized using Claisen–Schmidt condensation of p-hydroxyacetophenone with p-fluorobenzaldehyde
and p-bromobenzaldehyde using SOCl2/EtOH as a catalyst to obtain finally a fluorinated chalcone derivative (FCD) and a brominated
chalcone derivative (BCD) respectively.
These synthesized chalcones derivatives were esterified with ofloxacin to obtain two possible mutual prodrugs that evaluated for its
antibacterial activity against gram-positive and gram negative bacteria in comparison with standard antibiotics: ofloxacin and ciprofloxacin
using a disc diffusion method.
Results:
FTIR Spectroscopy, elemental microanalysis (CHN), and other physicochemical properties have been used to characterize the structure of the
synthesized compounds.A moderate antibacterial activity of the synthesized chalcone derivatives (FCD and BCD) was obtained whereas their
conjugates with ofloxacin were showed enhanced antibacterial activity in comparison with ofloxacin and ciprofloxacin using the culture and
sensitivity test model on gram-positive and negative bacteria.
Conclusion:
Chalcones with their pronounced antibacterial activity can enhance the activity of Fluoroquinolones when conjugated with this class of
antibiotics.
Keywords: Antibiotics, Fluoroquinolones, Ofloxacin, Chalcone derivatives, Mutual prodrugs.
