Some important chalcones have been prepared by condensing aryl ketones with aromatic aldehydes in presence of suitable condensing agents. The reactions have been carried out by conventional and green chemical techniques. These chalcones have been cyclised into benzodiazepines and their derivatives. The synthesized compounds were characterized by running TLC, elemental analysis, IR , 1HNMR and Mass spectroscopy. The prepared compounds have been screened for their spermicidal activity in semen of Holstein friesian cattle and antibacterial activity against Staphylococcus aureus, Escherichia coli ,Pseudomonas aeruginosa.