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New Nitrogen Containing Substituents at the Indole-2-carboxamide Yield High Potent and Broad Spectrum Indolylarylsulfone HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors

La Regina, G., Coluccia, Antonio, Brancale, Andrea, Piscitelli, F., Famiglini, V., Cosconati, S., Maga, G., Samuele, A., Gonzalez, E., Clotet, B., Schols, D., Este, J. A., Novellino, E. and Silvestri, R. 2012. New Nitrogen Containing Substituents at the Indole-2-carboxamide Yield High Potent and Broad Spectrum Indolylarylsulfone HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors. Journal of Medicinal Chemistry 55 (14) , pp. 6634-6638. 10.1021/jm300477h

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Abstract

New indolylarylsulfone (IAS) derivatives bearing nitrogen containing substituents at the indole-2-carboxamide inhibited the HIV-1 WT in MT-4 cells at low nanomolar concentrations. In particular, compound 9 was uniformly effective against the mutant Y181C, Y188L, and K103N HIV-1 strains; it was highly active against the multidrug resistant mutant IRLL98 HIV-1 strain bearing the K101Q, Y181C, and G190A mutations conferring resistance to NVP, DLV, and EFV and several HIV-1 clades A in PBMC.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RM Therapeutics. Pharmacology
Publisher: ACS Publications
ISSN: 0022-2623
Last Modified: 04 Jun 2017 04:32
URI: http://orca-mwe.cf.ac.uk/id/eprint/40765

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