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

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

Carmela Saturnino, Fedora Grande, Stefano Aquaro, Anna Caruso, Domenico Iacopetta, Maria Grazia Bonomo, Pasquale Longo, Dominique Schols, Maria Stefania Sinicropi

Molecules. 2018 Jan 30;23(2):286.

PMID: 29385738

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP51997514-A	4-(2-Oxiranylmethoxy)-9H-carbazole		51997-51-4	Price

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