Number of substituted 1, 5-benzodiazepines are known for their biological importance like anti-bacterial, antifungal, anticancer, and anti-inflammatory activity. The present investigation is carried for the synthesis of certain substituted 1, 5-benzodiazepines and carried out their sedative activity. The title compounds have been synthesized from OPD reacts with substituted aryl aldehydes to give substituted 1, 5-benzodiazepines. The newly synthesized compounds have been characterized by IR, 1H NMR and CHN analysis. Selected compounds are screened for sedative activity in vivo using spontaneous locomotor activity model. Few of them exhibited promising activity.