ウレアーゼ阻害剤による尿路結石の予防 第3報 : 新ヒドロキサム酸誘導体によるウレアーゼ阻害と膀胱結石形成の防止

Abstract

Hydroxamic acid, a potent and specific inhibitor of bacterial urease activity, was found to be effective for the prevention of alkalinization of infected urine and bladder stone formation. 1. Among new hydroxamic acid derivatives of hippuric acid, m-methoxyhippurohydroxamic acid (UCD II) was expected to be most effective, because of the strong inhibitory power against urease activity and the high urinary excretion in rats without degradation. 2. UCD II prevented the alkalinization of experimentally infected urine in vitro. 3. UCD II significantly prevented the bladder stone formation as well as alkalinization of urine in vivo, when the compound was orally administered to the rats with urinary tract infection caused by Proteus mirabilis. 4. Clinical application of UCD II was dependent upon the evaluation of safety of the compound, with reference to the prevention of pathologic sequelae of urinary infection with urease-producing bacteria.