Novel Cerebroprotective Agents with Central Nervous System Stimulating Activity. 1. Synthesis and Pharmacology of 1-Amino-7-hydroxyindan Derivatives

Article abstract of DOI:10.1021/jm00111a014

To developed a novel cerebroprotective agent with central nervous system (CNS) stimulating activity, a series of 1-amino-7-hydroxyindan derivatives was synthesized, and their effects on the survival time of mice under hypoxic conditions were tested.CNS-stimulating activity was also evaluated by examining the promotional effect on the recovery from cerebral concussion induced coma in mice.Several compounds prolonged the survival time of mice in hypoxic conditions at a dose of 30 mg/kg (sc or ip) and 100 mg/kg (po).They also exhibited the promotional effects on recovery from coma at a dose of 100 mg/kg po.The three most potent compounds in both tests, 1-amino-7-hydroxy-6-(1-methylpropyl)indan (20), 1-amino-7-hydroxy-4,6-dimethyl-2-phenylindan (30), and 1-amino-7-hydroxy,2,2,4,6-tetramethylindan (35) were selected for further investigations.Structure-activity relationships were also discussed.