AMINOOXYTETRAPHENYLPORPHYRINS AND HYDROXYTETRAPHENYLPORPHYRINS WITH ACTIVITY AGAINST THE HUMAN-IMMUNODEFICIENCY-VIRUS

A series of amino- and hydroxytetraphenylporphyrin derivatives was found to have activity against the human immunodeficiency virus type 1 (HIV-1) in human peripheral blood mononuclear cells. Activity tends to be associated with increased hydrophilicity of the porphyrins for the porphyrins with one substituent on each phenyl ring but there is no clear pattern for the porphyrins with two substituents on each phenyl ring. The antiviral activity of certain porphyrins has been demonstrated in the absence of light, suggesting a non-photochemical process. Whereas only some of the porphyrins that inhibit HIV-1 in culture inhibit HIV-1 reverse transcriptase in a cell-free system, none of those tested inhibit DNA polymerase-alpha.