Abstract: Since α-acetylaminoacetophenones are known to have antihepatitis activity, a series of aminoacyl and dipeptidyl derivatives were synthesized by replacement of the acetyl group with amino acid and dipeptide acyl groups or by changing the substituents on the benzene ring. Thirty-four compounds were submitted to pharmacological screen for antihepatitis and/or antipeptic ulcer activity. The results showed that the presence of methylene-dioxy group on the benzene ring showed favorable influence on the SGPT-lowering activity of the compounds.