Chloro-1,4-dimethyl-9H-carbazole Derivatives Displaying Anti-HIV Activity.

Background: 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.
Methods: Six chloro-1,4-dimethyl-9 H -carbazoles ( 2a , b - 4a , b ) have been prepared following opportunely modified known chemical procedures and tested in luciferase and Escherichia coli β-galactosidase expressing CD4⁺, CXCR4⁺, CCR5⁺ TZM-bl cells.
Results and Conclusion: a preliminary biological investigation on the synthesized small series of chloro-1,4-dimethyl-9 H -carbazoles has been carried out. Among all tested compounds, a nitro-derivative ( 3b ) showed the most interesting profile representing a suitable lead for the development of novel anti-HIV drugs.
Competing Interests: The authors declare no conflict of interest.