New Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors Show Low Nanomolar Inhibition of Single and Double HIV-1 Mutant Strains

Marianna Nalli,Jorge I. Armijos Rivera,Domiziana Masci,Antonio Coluccia,Roger Badia,Eva Riveira-Muñoz,Alessandro Brambilla,Elisabetta Cinquina,Ombretta Turriziani,Francesca Falasca,Myriam Catalano,Cristina Limatola,José A. Esté,Giovanni Maga,Romano Silvestri,Emmanuele Crespan,Giuseppe La Regina

New Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors Show Low Nanomolar Inhibition of Single and Double HIV-1 Mutant Strains

2020

Marianna Nalli
Jorge I. Armijos Rivera
Domiziana Masci
Antonio Coluccia
Roger Badia
Eva Riveira-Muñoz
Alessandro Brambilla
Elisabetta Cinquina
Ombretta Turriziani
Francesca Falasca
Myriam Catalano
Cristina Limatola
José A. Esté
Giovanni Maga
Romano Silvestri
Emmanuele Crespan
Giuseppe La Regina

Abstract We designed and synthesized 21 new indolylarylsulfones (IAS) as new HIV-1 NNRTIs. Among these, IAS 12 exhibited a remarkable antiviral activity against single and double mutants (K103N EC50:

Keywords:

Chemistry
Nucleoside Reverse Transcriptase Inhibitor
Mutant
Virology
human immunodeficiency virus

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