Abstract: Glycine transporter-1 (GlyT1) is an attractive therapeutic target for schizophrenia.A series of novel quinazolone derivatives were designed and synthesized as active GlyT1 inhibitors on the basis of compound 2,4-dichloro-N-4-(cyclopropylmethyl)-1-(ethylsulfonyl)piperidin-4-ylmethylbenzamide( 1a ,IC₅₀=92.2 nmol/L)developed by Merck & Co Inc.Preliminary results showed that all the compounds except 7e possessed GlyT1 inhibitory activity to a different extent,and that compound 7j was the most potent one within this series of compounds,possessing almost the same potency as that of compound 1a .