Infectious

In vitro and cell culture studies identified a heteroarylpropanediamine-based CCR5 antagonist that could help treat HIV-1 infection. Chemical synthesis and in vitro testing in enzymatic activity assays of a series of 1-heteroaryl-1,3-propanediamine analogs yielded a compound that antagonized CCR5 with an IC₅₀ of 3 nM. In an HIV-1 reporter cell line, the compound decreased HIV-1 infectivity compared with the CCR5 antagonist Selzentry maraviroc. In human peripheral blood mononuclear cells and a human T lymphoid cell line infected with HIV-1 isolates, the compound decreased infectivity. Next steps could include testing the compound in animal models of HIV-1 infection...