Potential new anti-human immunodeficiency virus type 1 compounds depress virus replication in cultured human macrophages.

We report that the amiloride analogues 5-(N,N'-hexamethylene)amiloride and 5-(N,N'-dimethyl)amiloride inhibit, at micromolar concentrations, the replication of human immunodeficiency virus type 1 (HIV-1) in cultured human blood monocyte-derived macrophages. These compounds also inhibit the in vitro activities of the HIV-1 Vpu protein and might represent lead compounds for a new class of anti-HIV-1 drugs.