A novel synthesis of somatostatin mimetics based on the 1-deoxymannojirimycin (DMJ) scaffoldhas been developed. This involved development of a route suitable for the strategic grafting ofpharmacophoric tryptophan and lysine side chains to the nitrogen atom of the piperidine ring andto the primary hydroxyl group of DMJ, respectively. The novel peptidomimetics were found to bindwith higher affinity to sst4 receptors than to sst5 receptors.