Synthesis and Antidepressant Activity of 2, 3, 4, 5-­‐Tetrahydro-­‐1H-­‐1, 4-­‐ benzodiazepine Derivatives

Abstract

Benzodiazepines    are    wide    range    pharmacological    activities.    Compounds    containing    substituted    1,4-­‐ dibenzoazepine have received attention of potent axiolytic agents. We synthesized 2, 3, 4, 5-­‐tetrahydro-­‐1H-­‐1, 4-­‐ benzodiazepine derivatives from isatoic acid anhydride. Based on the evaluation of antidepressant and antiepileptic  activities,  the  compound,  4-­‐benzyl-­‐2,  3,  4,  5-­‐tetrahydro-­‐1H-­‐1,  4-­‐benzodiazepine  (BZD5)  and  4-­‐(4-­‐ nitrobenzyl)-­‐2,   3,   4,   5-­‐tetrahydro-­‐1H-­‐1,   4-­‐benzodiazepine   (BZD6)   were   identified   as   potent   and   safe   novel antidepressant  molecule.  All  compounds  were  tested  in  different  doses  2.5,  5.0  and  10.0   mg/kg,   inform   both forced swimming immobility test and tail suspension test. The  compound  BZD5  was  more  effective  and  higher significance than the reference drug, phenelpazine (10 mg/kg, IP).