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 ORCID: https://orcid.org/0000-0002-9728-3419, 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:	05 Jan 2024 05:53
URI:	https://orca.cardiff.ac.uk/id/eprint/40765

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