An evaluation of spirooxindoles as blocking agents of SARS-CoV-2 spike/ACE2 fusion and M pro inhibitory agents: Synthesis, biological evaluation and computational analysis
Albert Enama Ehinak,
Maloba M. M. Lobe,
Conrad V. Simoben
et al.
Abstract:Both tetrahydroisoquinolines (THIQs) and oxindoles (OXs) display a broad range of biological activities, including antiviral activity. They are, therefore, recognized as privileged scaffolds in drug discovery. Here, we describe the synthesis of spirofused tetrahydroisoquinoline–oxindole hybrids (spirooxindoles) and their evaluation as potential blocking agents of both SARS-CoV-2 spike/ACE fusion and inhibitors of the main protease (Mpro). The most active synthesized compound showed a 50% inhibitory concentrati… Show more
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