Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
404.017048324
InChI
InChI=1S/C14H16N2O6S3/c17-23(18)9-15-11-1-5-13(6-2-11)25(21,22)14-7-3-12(4-8-14)16-10-24(19)20/h1-8,15-16H,9-10H2,(H,17,18)(H,19,20)
InChI Key
InChIKey=NEDPPCHNEOMTJV-UHFFFAOYSA-N
IUPAC Name
{[4-({4-[(sulfinomethyl)amino]benzene}sulfonyl)phenyl]amino}methanesulfinic acid
Traditional IUPAC Name
[(4-{4-[(sulfinomethyl)amino]benzenesulfonyl}phenyl)amino]methanesulfinic acid
SMILES
OS(=O)CNC1=CC=C(C=C1)S(=O)(=O)C1=CC=C(NCS(O)=O)C=C1
pKa (strongest acidic)
-1.5
pKa (Strongest Basic)
-0.056
Refractivity
96.95 m3·mol-1
Dược Lực Học :
Sulfoxone 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 :
Sulfoxone is a water-soluble sulfone used as an antileprosy drug. It has been used with limited success in the treatment of dermatitis herpetiformis.
Sulfoxone is a competitive inhibitor of bacterial enzyme dihydropteroate synthetase. The normal substrate for the enzyme, para-aminobenzoic acid (PABA) cannot bind as usual. The inhibited reaction is necessary in these organisms for the synthesis of folic acid.
Dược Động Học :
▧ Absorption :
Rapidly absorbed.
▧ Protein binding :
69%
▧ Metabolism :
Hepatic.
▧ Half Life :
3-8 hours
Độc Tính :
Oral, rat LD50: 7000 mg/kg
Chỉ Định :
For the treatment of leprosy and dermatitis herpetiformis