SP inhibitor 1 (compound 34) is a selective SARS-CoV-2 spike protein (SP) inhibitor with an IC 50 of 3.26 μM, >25 μM, >25 μM for SP, M pro and PL pro protein, respectively. SP inhibitor 1 is a vitro SARS-CoV-2 replication inhibitor at non-toxic concentrations (0.32 50<5.98 μM). SP inhibitor 1 shows cellular antiviral activity.