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药品详细

Acetohydroxamic Acid(乙酰氧肟酸)

化学结构式图
中文名
乙酰氧肟酸
英文名
Acetohydroxamic Acid
分子式
C2H5NO2
化学名
N-hydroxyacetamide
分子量
Average: 75.0666
Monoisotopic: 75.032028409
CAS号
546-88-3
ATC分类
G04B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Acetohydroxamic Acid, a synthetic drug derived from hydroxylamine and ethyl acetate, is similar in structure to urea. In the urine, it acts as an antagonist of the bacterial enzyme urease. Acetohydroxamic Acid has no direct antimicrobial action and does not acidify urine directly. It is used, in addition to antibiotics or medical procedures, to treat chronic urea-splitting urinary infections.

生产厂家
  • Mission pharmacal co
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Link
剂型
规格
化合物类型
Type small molecule
Classes
  • Amino Ketones
Substructures
  • Hydroxy Compounds
  • Hydroxamic Acids
  • Amino Ketones
  • Carboxamides and Derivatives
适应症
药理
Indication Used, in addition to antibiotics or medical procedures, to treat chronic urea-splitting urinary infections.
Pharmacodynamics Acetohydroxamic Acid, a synthetic drug derived from hydroxylamine and ethyl acetate, is similar in structure to urea. In the urine, it acts as an antagonist of the bacterial enzyme urease. Acetohydroxamic Acid has no direct antimicrobial action and does not acidify urine directly.
Mechanism of action Acetohydroxamic Acid reversibly inhibits the bacterial enzyme urease. This inhibits the hydrolysis of urea and production of ammonia in urine infected with urea-splitting organisms, leading to a decrease in pH and ammonia levels. As antimicrobial agents are more effective in such conditions, the effectiveness of these agents is amplified, resulting in a higher cure rate.
Absorption Well absorbed from the GI tract following oral administration.
Volume of distribution Not Available
Protein binding No known binding
Metabolism
35-65% of oral dose excreted unchanged in urine (which provides the drug's therapeutic effect).
Route of elimination Not Available
Half life 5-10 hours in patients with normal renal function
Clearance Not Available
Toxicity Oral, rat: LD50 = 4.8gm/kg. Symptoms of overdose include anorexia, malaise, lethargy, diminished sense of wellbeing, tremor, anxiety, nausea, and vomiting.
Affected organisms
  • Enteric bacteria and other eubacteria
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 90.5 °C PhysProp
water solubility 1E+006 mg/L Not Available
logP -1.59 HANSCH,C ET AL. (1995)
pKa 8.7 (at 25 °C) SERJEANT,EP & DEMPSEY,B (1979)
Predicted Properties
Property Value Source
water solubility 5.09e+02 g/l ALOGPS
logP -1.5 ALOGPS
logP -1 ChemAxon
logS 0.83 ALOGPS
pKa (strongest acidic) 8.94 ChemAxon
pKa (strongest basic) -5.4 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 2 ChemAxon
polar surface area 49.33 ChemAxon
rotatable bond count 0 ChemAxon
refractivity 16.23 ChemAxon
polarizability 6.6 ChemAxon
药物相互作用
食物相互作用
Not Available

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