Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
249.111341361
InChI
InChI=1S/C12H15N3O3/c1-3-6-18-8-4-5-9-10(7-8)14-11(13-9)15-12(16)17-2/h4-5,7H,3,6H2,1-2H3,(H2,13,14,15,16)
InChI Key
InChIKey=RAOCRURYZCVHMG-UHFFFAOYSA-N
IUPAC Name
methyl N-(6-propoxy-1H-1,3-benzodiazol-2-yl)carbamate
Traditional IUPAC Name
oxibendazole
SMILES
CCCOC1=CC2=C(C=C1)N=C(NC(=O)OC)N2
pKa (strongest acidic)
9.64
pKa (Strongest Basic)
4.56
Refractivity
66.66 m3·mol-1
Cơ Chế Tác Dụng :
Oxibendazole is a polymerase inhibitor in phase III trials for the treatment of helminth intestinal infections.
Oxibendazole causes degenerative alterations in the tegument and intestinal cells of the worm by binding to the colchicine-sensitive site of tubulin, thus inhibiting its polymerization or assembly into microtubules. The loss of the cytoplasmic microtubules leads to impaired uptake of glucose by the larval and adult stages of the susceptible parasites, and depletes their glycogen stores. Degenerative changes in the endoplasmic reticulum, the mitochondria of the germinal layer, and the subsequent release of lysosomes result in decreased production of adenosine triphosphate (ATP), which is the energy required for the survival of the helminth. Due to diminished energy production, the parasite is immobilized and eventually dies.
Dược Động Học :
▧ Metabolism :
Hepatic
Chỉ Định :
Investigated for use/treatment in infectious and parasitic disease (unspecified) and pediatric indications.