Fluoroquinolones as Urease Inhibitors: Anti-Proteus mirabilis Activity and Molecular Docking Studies

Mohammed A. A. Abdullah¹, Rehab M. Abd El-Baky^2, , Heba A. Hassan¹, El-Shimaa M. N. Abdelhafez¹ and Gamal El-Din A. Abuo-Rahma¹

¹Departement of Medicinal Chemistry, Faculty of Pharmacy, Minia University, Minia, Egypt

²Departement of Microbiology and Immunology, Faculty of Pharmacy, Minia University, Minia, Egypt

Cite this paper:
Mohammed A. A. Abdullah, Rehab M. Abd El-Baky, Heba A. Hassan, El-Shimaa M. N. Abdelhafez and Gamal El-Din A. Abuo-Rahma. Fluoroquinolones as Urease Inhibitors: Anti-Proteus mirabilis Activity and Molecular Docking Studies. American Journal of Microbiological Research. 2016; 4(3):81-84. doi: 10.12691/ajmr-4-3-3

Abstract

The anti-Proteus mirabilis activity and MIC of levofloxacin and ciprofloxacin were investigated in comparison with the known urease inhibitor acetohydroxamic acid using Well Diffusion method. Also, their inhibitory effect on urease was determined by measuring ammonia production as an indicator of urease activity using the indophenol method as described by Weatherburn. AHA showed a weak anti-Proteus mirabilis activity the (MIC = 614.8 µM) than the two tested fluoroquinolones (MIC for levofloxacin = 3.2 µM and for ciprofloxacin = 15.62 µM). The tested fluoroquinolones experienced excellent urease inhibitory activity IC₅₀ for levofloxacin = 2.9 µM and for ciprofloxacin = 3.5 µM). However, the results were supported by molecular docking studies to gain insights into the binding conformations as well as the inhibition mode of urease and showed coordination binding with the two Ni ion in the active site which are essential for urea breakdown.

Keywords:
Flurorquionolones Urease inhibition Anti-Proteus mirabilis Docking

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