A series of aromatic, water soluble and non-toxic amino acid phosphoramidate di- and triesters of zidovudine (AZT) were shown to inhibit the replication of HIV-1 in human peripheral blood mononuclear cells (PBMC). Cells treated with the active AZT diesters contained four fold more phosphorylated AZT than those treated with AZT, and no free AZT.