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Molecules 2018, 23(2), 286; https://doi.org/10.3390/molecules23020286

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

1
Department of Science, University of Basilicata, 85100 Potenza, Italy
2
Department of Pharmacy, Health & Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende, Italy
3
Department of Chemistry and Biology, University of Salerno, 84084 Fisciano, Italy
4
KU Leuven, Rega Institute for Medical Research, Herestraat 49, B-3000 Leuven, Belgium
*
Authors to whom correspondence should be addressed.
Received: 21 December 2017 / Revised: 18 January 2018 / Accepted: 27 January 2018 / Published: 30 January 2018
(This article belongs to the Section Medicinal Chemistry)
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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,b4a,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. View Full-Text
Keywords: carbazole derivatives; HIV; antiviral agents carbazole derivatives; HIV; antiviral agents
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Saturnino, C.; Grande, F.; Aquaro, S.; Caruso, A.; Iacopetta, D.; Bonomo, M.G.; Longo, P.; Schols, D.; Sinicropi, M.S. Chloro-1,4-dimethyl-9H-carbazole Derivatives Displaying Anti-HIV Activity. Molecules 2018, 23, 286.

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