A single oral administration of the urease inhibitor benurestat (2-(p-chlorobenz-amido)acetohydroxamic acid) to the human at 15 or 25 mg per kg produced, for 4 hr, mean urinary levels of inhibitory activity that were 700 to 1900 times that equivalent concentration of benurestat required to inhibit Proteus mirabilis urease by 90 per cent. In the rat these same dosage levels produced urinary inhibitory activity equivalent to 16 to 140 fold that required for 90 per cent urease inhibition. Benurestat administration, 25, 50, or 100 mg per kg, caused a decrease in the urinary excretion of ammonia from rats with experimental P. mirabilis genitourinary tract infection. The formation of struvite calculi was inhibited under these conditions. Nitrofurantoin, sulfamethoxazole, and ampicillin also slowed the formation of struvite calculi in infected rats and together with benurestat a potentiation of the inhibition of calculi formation was secured. Some combination therapies composed of benurestat plus an antibacterial agent, sulfamethoxazole or ampicillin, were effective in promoting the net dissolution of formed calculi. The number of viable bacteria present in the bladders of infected rats was significantly less after the administration of benurestat plus nitrofurantoin, sulfamethoxazole, or ampicillin than the respective numbers that were obtained from control infected rats or from rats administered either component of the combination separately.

中文翻译：

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Benurestat，一种脲酶抑制剂，用于治疗感染的尿素溶解。

以每公斤15或25 mg的剂量向人单次口服脲酶抑制剂benurestat（2-（对-氯苯甲酰胺基）乙酰氧肟酸）4小时，尿液平均抑制活性为700至1900倍相当于必须将贝那司他的等效浓度抑制90％的奇异变形杆菌尿素酶。在大鼠中，这些相同的剂量水平产生的尿抑制活性相当于90％的尿素酶抑制所需要的16至140倍。每公斤25、50或100毫克的Benurestat给药导致实验性狂犬性泌尿生殖道泌尿道感染的大鼠尿中氨的排泄减少。在这些条件下鸟粪石结石的形成受到抑制。呋喃妥因，磺胺甲恶唑，氨苄西林还可以减缓感染的大鼠中鸟粪石结石的形成，并与苯那司他合用可以确保抑制结石的形成。由benurestat加上抗菌剂，磺胺甲恶唑或氨苄青霉素组成的某些联合疗法可有效促进结石的净溶解。给予倍尼司他加硝基呋喃妥因，磺胺甲恶唑或氨苄青霉素后，感染大鼠膀胱中存在的活菌数量明显少于对照感染大鼠或单独给予该组合中任一组分的大鼠。磺胺甲恶唑或氨苄青霉素可有效促进结石的净溶解。给予倍尼司他加硝基呋喃妥因，磺胺甲恶唑或氨苄青霉素后，感染大鼠膀胱中存在的活菌数量明显少于对照感染大鼠或单独给予该组合中任一组分的大鼠。磺胺甲恶唑或氨苄青霉素可有效促进结石的净溶解。给予倍尼司他加硝基呋喃妥因，磺胺甲恶唑或氨苄青霉素后，感染大鼠膀胱中存在的活细菌数量明显少于对照感染大鼠或单独给予该组合中任一组分的大鼠。