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- Title
Chloro-1,4-dimethyl-9H-carbazole Derivatives Displaying Anti-HIV Activity.
- Authors
Saturnino, Carmela; Grande, Fedora; Aquaro, Stefano; Caruso, Anna; Iacopetta, Domenico; Bonomo, Maria Grazia; Longo, Pasquale; Schols, Dominique; Sinicropi, Maria Stefania
- 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 -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.
- Subjects
ANTIRETROVIRAL agents; ANTIVIRAL agents; HIV prevention; DRUG development; CARBAZOLE
- Publication
Molecules, 2018, Vol 23, Issue 2, p286
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules23020286