Systematic investigation of the amino acid sidechain of L-692,429, the prototype of a novel class of benzolactam growth hormone (GH) secretagogues, has led to the preparation of L-692,585, a 2(R)hydroxypropyl amino analog, which is twenty times more potent in vitro than L-692,429. Additional amino modifications reported here further define the structure-activity profile for L-692,429.