Abstract
Several 4'-substituted pyridoxine (PN) analogues were synthesized and the antivitamin B_6 activities were tested using Saccharomyces carlsbergensis and mouse. 4'-Methoxy PN (4'-MPN), 4'-ethoxy PN (4'-EPN), 4'-propoxy PN (4'-PPN) and 4'-isopropoxy PN (4'-isoPPN) showed a slight antivitamin B_6 activities for S. carls., but found to be more potent antivitamin B_6 than 4'-deoxy PN (4'-DPN) for mouse. These analogues induced the characteristic convulsions at the intraperitoneal dose of 0.05 mmol/kg, 0.08 mmol/kg, 0.20 mmol/kg and 0.44 mmol/kg, respectively. The convulsions were prevented by the administration of PN and PLP. In rats, 64% of 4'-PPN administered orally or intraperitoneally were excreted in the urine within 24 hours and 4'-PPN 3-sulfate was estimated as a metabolite in the urine.
