Abstract
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-9H-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-9H-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.
Highlights
Nowadays, according to the National Institute on Drug Abuse (NIDA), part of the National Institutes of Health, approximately 37 million people are infected with HIV worldwide
Starting from the commercially available indoles 1a–b, the corresponding carbazole derivatives 2a–b were synthesized according to the method of Cranwell and Saxton [38]
These intermediates were transformed into the nitro derivatives 3a–b that were in turn reduced by stannous chloride to furnish the 3-amino-1,4-dimethyl-9H-carbazoles 4a–b with good yields (Scheme 1) [39]
Summary
The most clinically adopted treatment consists in a combination of three anti-HIV drugs from at least two different classes in order to inhibit viral replication and diminish the onset of drug resistance [2]. This approach has resulted in a significant decrease of viral replication in HIV-infected individuals as well as a reduction of the risk of viral transmission [3,4]. 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. A nitro-derivative (3b) showed the most interesting profile representing a suitable lead for the development of novel anti-HIV drugs.
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