Effective control of the replication of HIV virus has been in focus for decades. In an attempt to control the HIV replication, our approach is to inhibit the Tat-TAR interaction. We have attempted to synthesize analogues to bind specifically to the transactivator protein, Tat. In this poster, details of the synthesis of arginine analogues will be presented. Experiments for the investigation of the toxicity and anti-HIV activity are underway.