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药品详细

Sulfamoxole(Sulfamoxole)

化学结构式图
中文名
Sulfamoxole
英文名
Sulfamoxole
分子式
C11H13N3O3S
化学名
4-amino-N-(dimethyl-1,3-oxazol-2-yl)benzene-1-sulfonamide
分子量
Average: 267.304
Monoisotopic: 267.067761987
CAS号
729-99-7
ATC分类
J01E 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Sulfamoxole is a sulfonamide antibacterial.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. DUGGER JA: Sulfamoxole (Nuprin), a new sulfonamide, in pediatric practice. J New Drugs. 1961 Sep-Oct;1:223-9. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes Not Available
    Substructures Not Available
    适应症
    药理
    Indication For the treatment of bacterial infection.
    Pharmacodynamics Sulfamoxole is a sulfonamide antibiotic. The sulfonamides are synthetic bacteriostatic antibiotics with a wide spectrum against most gram-positive and many gram-negative organisms. However, many strains of an individual species may be resistant. Sulfonamides inhibit multiplication of bacteria by acting as competitive inhibitors of p-aminobenzoic acid in the folic acid metabolism cycle. Bacterial sensitivity is the same for the various sulfonamides, and resistance to one sulfonamide indicates resistance to all. Most sulfonamides are readily absorbed orally. However, parenteral administration is difficult, since the soluble sulfonamide salts are highly alkaline and irritating to the tissues. The sulfonamides are widely distributed throughout all tissues. High levels are achieved in pleural, peritoneal, synovial, and ocular fluids. Although these drugs are no longer used to treat meningitis, CSF levels are high in meningeal infections. Their antibacterial action is inhibited by pus.
    Mechanism of action Sulfamoxole is a competitive inhibitor of the bacterial enzyme dihydropteroate synthetase. This enzyme is needed for the proper processing of para-aminobenzoic acid (PABA) which is essential for folic acid synthesis. The inhibited reaction is necessary in these organisms for the synthesis of folic acid.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity Oral Rat LD50: > 12500 mg/kg; Intravenous Mouse LD50: 1 g/kg
    Affected organisms
    • Enteric bacteria and other eubacteria
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 193 °C PhysProp
    water solubility 1680 mg/L (at 20 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
    Predicted Properties
    Property Value Source
    water solubility 2.67e-01 g/l ALOGPS
    logP 1.04 ALOGPS
    logP 0.59 ChemAxon
    logS -3 ALOGPS
    pKa (strongest acidic) 6.81 ChemAxon
    pKa (strongest basic) 1.94 ChemAxon
    physiological charge -1 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 98.22 ChemAxon
    rotatable bond count 2 ChemAxon
    refractivity 67.51 ChemAxon
    polarizability 27.44 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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