Herein, we disclose a general and flexible access to spirocyclopropyl oxindoles by a domino Michael/intramolecular nucleophilic substitution pathway with variously substituted vinyl selenones and enolizable oxindoles in aqueous sodium hydroxide solution. The spirocyclopropyl oxindole being a privileged scaffold, some of the synthesized compounds were selected for biological evaluation. Compound 3m showed selective anti-HIV-1 activity thanks to its ability to inhibit the reverse transcriptase.

A new vinyl selenone-based domino approach to spirocyclopropyl oxindoles endowed with anti-HIV RT activity

Tramontano, E.;Corona, A.;
2016

Abstract

Herein, we disclose a general and flexible access to spirocyclopropyl oxindoles by a domino Michael/intramolecular nucleophilic substitution pathway with variously substituted vinyl selenones and enolizable oxindoles in aqueous sodium hydroxide solution. The spirocyclopropyl oxindole being a privileged scaffold, some of the synthesized compounds were selected for biological evaluation. Compound 3m showed selective anti-HIV-1 activity thanks to its ability to inhibit the reverse transcriptase.
HIV; Reverse transcriptase; Inhibition; Virus
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11584/175723
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