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Despite the progress achieved by anti-retroviral drug research in the last decades, the discovery of novel compounds endowed with selective antiviral activity and reduced side effects is still a necessity. At present, the most urgent requirement includes the improvement of HIV (Human Immunodeficiency Virus) prevention and sexual transmission and the development of new drugs to treat the chronic lifelong infection.
Six chloro-1,4-dimethyl-9
-carbazoles (
,
-
,
) have been prepared following opportunely modified known chemical procedures and tested in luciferase and
β-galactosidase expressing CD4⁺, CXCR4⁺, CCR5⁺ TZM-bl cells.
a preliminary biological investigation on the synthesized small series of chloro-1,4-dimethyl-9
-carbazoles has been carried out. Among all tested compounds, a nitro-derivative (
) showed the most interesting profile representing a suitable lead for the development of novel anti-HIV drugs.