Acetohydroxamic acid (AHA)

Acetohydroxamic acid (AHA) is an irreversible inhibitor of urease and a derivative of hydroxyurea .¹ It inhibits the growth of struvite crystals produced by P. mirabilis in artificial urine and the growth of H. pylori in vitro (MICs = 200 and 400 mg/L for various isolates of H. pylori).^2,3 Chronic AHA administration in dogs dose-dependently reduces urine urease activity, pH, and crystalluria and inhibits growth of bladder stones.⁴ It also decreases gastritis, gastric lesions, and bacterial infection rates in Mongolian gerbils when administered at 2,500 ppm/animal following H. pylori infection.⁵ Formulations containing AHA have been used in the treatment of urinary tract infections.

1.Fishbein, W.N., and Carbone, P.P.Urease Catalysis. II. Inhibition of the enzyme by hydroxyurea, hydroxylamine, and acetohydroxamic acidJ. Biol. Chem.240(6)2407-2414(1965) 2.Downey, J.A., Nickel, J.C., Clapham, L., et al.In vitro inhibition of struvite crystal growth by acetohydroxamic acidBr. J. Urol.70(4)355-359(1992) 3.Phillips, K., Munster, D.J., Allardyce, R.A., et al.Antibacterial action of the urease inhibitor acetohydroxamic acid on Helicobacter pyloriJ. Clin. Pathol.46(4)372-373(1993) 4.Krawiec, D.R., Osborne, C.A., Leininger, J.R., et al.Effect of acetohydroxamic acid on dissolution of canine struvite urolithsAm. J. Vet. Res.45(7)1266-1275(1984) 5.Ohta, T., Shibata, H., Kawamori, T., et al.Marked reduction of Helicobacter pylori-induced gastritis by urease inhibitors, acetohydroxamic acid and flurofamide, in Mongolian gerbilsBiochem. Biophys. Res. Commun.285(3)728-733(2001)