Flurofamide: a potent inhibitor of bacterial urease with potential clinical utility in the treatment of infection induced urinary stones.

  title={Flurofamide: a potent inhibitor of bacterial urease with potential clinical utility in the treatment of infection induced urinary stones.},
  author={O. Elmo Millner and J A Andersen and Matthew Appler and C. Benjam{\'i}n and John G. Edwards and D T Humphrey and E M Shearer},
  journal={The Journal of urology},
  volume={127 2},
AbstractA novel compound, N-[diaminophosphinyl]-4-fluorobenzamide (given the USAN name flurofamide), has been found to be a potent inhibitor of bacterial urease. The compound, coded EU-4534, is approximately 1000 times more potent than acetohydroxamic acid as an inhibitor of the urease in intact P. mirabilis cells. Flurofamide is excreted in the urine of rats and dogs following oral administration and is effective in retarding stone formation in the urinary tract of rats infected with P… 
Effect of Potent Urease Inhibitor, Fluorofamide, on Helicobacter sp. in Vivo and in Vitro
It was concluded that urease inhibitors either alone or in combination with antibiotics are unlikely to have therapeutic potential for Helicobacter pylori infections, probably because, in vivo, some bacteria (perhaps dormant forms) are not entirely dependent upon Urease for survival.
Investigation into the inhibitory effect of flurofamide on animal ureaplasmas and its use in the treatment of ureaplasma-infected sheep.
In vitro tests with the urease inhibitor flurofamide demonstrated that the final inhibitory concentration of 0.5-4 microM on the growth of nine ureaplasma strains was largely ureaplasmastatic,
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    The Yale journal of biology and medicine
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Flurofamide (N-[diaminophosphinyl]-4-fluorobenzamide), a urease inhibitor, was a potent inhibitor of the growth of Ureaplasma urealyticum. As little as 10 microM flurofamide (2 micrograms/ml)
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  • 2010
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Relative Merit of Various Nonsurgical Treatments of Infection Stones in Dogs
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The Role of Purified Urease from Proteus Mirabilis PMS17 in Stones Formation
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Urease activity is a physiological function of many bacteria that enables these organisms to utilize urea as a source of nitrogen. The association of ureolytic bacteria with human or animal hosts
Inhibition of urease activity in the urinary tract pathogen Staphylococcus saprophyticus
Results suggest that urease inhibitors may be useful for treating urinary tract infections caused by Staph.
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The Urease of C. pylori appears to be biochemically unique from the enzymes of other common urease-producing species.
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Acetohydroxamic acid, a potent inhibitor of urease, has been administered to 23 patients with staghorn renal calculi and urea-splitting urinary infection and has been well tolerated and effective for 2 to 12 months, even in patients with impaired renal function.
Influence of acetohydroxamic acid on experimental Corynebacterium renale pyelonephritis.
The role of Corynebacterium renale urease in the establishment of pyelonephritis was studied by the oral administration of acetohydroxamic acid (AHA) to experimentally infected rats and larger doses, given by gavage, did accomplish this goal.
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Previous reports have suggested that urease-producing bacteria play a prominent role in the formation of infection-induced urinary stones. We have carried out crystalization experiments in vitro
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Long-term chemotherapy with antimicrobial agents that achieve sterile urine or acetohydroxamic acid in those patients with recalcitrant infection lessens the risk of recurrent calculogenesis.
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It can be shown, on the basis of any rate theory that assumes the existence of an equilibrium of activation, that the substrate in its passage to product acquires a fleeting, but greatly elevated, affinity for the enzyme.
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A microdiffusion method for the determination of ammonia, which employs a simple diffusion cell and a mechanical rotator, is described, which has proved simple, rapid, and accurate.
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