Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
267.067761987
InChI
InChI=1S/C11H13N3O3S/c1-7-8(2)17-11(13-7)14-18(15,16)10-5-3-9(12)4-6-10/h3-6H,12H2,1-2H3,(H,13,14)
InChI Key
InChIKey=CYFLXLSBHQBMFT-UHFFFAOYSA-N
IUPAC Name
4-amino-N-(dimethyl-1,3-oxazol-2-yl)benzene-1-sulfonamide
Traditional IUPAC Name
sulfamoxole
SMILES
CC1=C(C)N=C(NS(=O)(=O)C2=CC=C(N)C=C2)O1
Độ hòa tan
1680 mg/L (at 20 °C)
pKa (strongest acidic)
6.81
pKa (Strongest Basic)
1.94
Refractivity
67.51 m3·mol-1
Dược Lực Học :
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.
Cơ Chế Tác Dụng :
Sulfamoxole is a sulfonamide antibacterial.
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.
Độc Tính :
Oral Rat LD50: > 12500 mg/kg; Intravenous Mouse LD50: 1 g/kg
Chỉ Định :
For the treatment of bacterial infection.