The antibacterial action and MIC of two newly synthesized fluoroquinolones hydroxamic acid derivatives 1 and 2 were investigated against Proteus mirabilis using Well Diffusion method. Moreover, their effect on urease activity was determined by measuring ammonia production, as indicator of urease activity, using the indophenol method as described by Weatherburn, 1967. Also, results were supported by molecular docking studies to gain insights into the binding conformations as well as the inhibition mode of urease. The target compounds showed a weaker anti-Proteus mirabilis than their parent fluoroquinolones. On the other hand, they showed a potent urease inhibition in comparison with Acetohydroxamic (AHA). The IC50 (µM) was found to be 2.2±0.04 for compound 1 and 2.22±0.21 for Compound 2, while the IC50 of AHA is 120±0.06. Therefore, these two new hydroxamic acids represent promising candidates for the treatment of urease-related complications.

New fluoroquinolone hydroxamic acids as antibacterial and urease inhibitors: Design, synthesis and molecular docking studies

251st National Meeting (2016)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.