Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
249.057197301
InChI
InChI=1S/C11H11N3O2S/c12-9-4-6-10(7-5-9)17(15,16)14-11-3-1-2-8-13-11/h1-8H,12H2,(H,13,14)
InChI Key
InChIKey=GECHUMIMRBOMGK-UHFFFAOYSA-N
IUPAC Name
4-amino-N-(pyridin-2-yl)benzene-1-sulfonamide
Traditional IUPAC Name
sulfapyridine
SMILES
NC1=CC=C(C=C1)S(=O)(=O)NC1=CC=CC=N1
Độ hòa tan
268 mg/L (at 25 °C)
pKa (strongest acidic)
6.24
pKa (Strongest Basic)
2.63
Refractivity
65.75 m3·mol-1
Dược Lực Học :
Sulfapyridine 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 :
Antibacterial, potentially toxic, and previously used to treat certain skin diseases. No longer prescribed.
Sulfapyridine is a competitive inhibitor of the bacterial enzyme dihydropteroate synthetase. The inhibited reaction is necessary in these organisms for the synthesis of folic acid by means of processing the substrate para-aminobenzoic acid (PABA). Dihydropteroate synthetase activity is vital in the synthesis of folate, and folate is required for cells to make nucleic acids, such as DNA or RNA. So if DNA molecules cannot be built, the cell cannot divide.
Dược Động Học :
▧ Absorption :
Approximately 60-80%
▧ Protein binding :
Approximately 50% bound to plasma proteins.
▧ Metabolism :
Hepatic.
▧ Half Life :
6-14 hours.
Độc Tính :
LD50 is 15800 mg/kg (orally in rats).
Chỉ Định :
For the treatment of dermatitis herpetiformis, benign mucous membrane pemphigoid and pyoderma gangrenosum
Dữ Kiện Thương Mại
Giá thị trường
-
Giá bán buôn : USD >0.13
Đơn vị tính : g