biostudies-literatureUnknown15(2)Wang XThe ongoing COVID-19 pandemic has caused over six million deaths and huge economic burdens worldwide. Antivirals against its causative agent, SARS-CoV-2, are in urgent demand. Previously, we reported that heterocylic compounds, i.e., chloroquine (CQ) and hydroxychloroquine (HCQ), are potent in inhibiting SARS-CoV-2 replication <i>in vitro</i>. In this study, we discussed the syntheses of two novel heterocylic compounds: <i>tert</i>-butyl <i>rel</i>-4-(((3<i>R</i>,4<i>S</i>)-3-(1<i>H</i>-indol-3-yl)-1-oxo-2-propyl-1,2,3,4-tetrahydroisoquinolin-4-yl)methyl)piperazine-1-carboxylate (<i>trans</i>-<b>1</b>) and <i>rel</i>-(3<i>R</i>,4<i>S</i>)-3-(1<i>H</i>-indol-3-yl)-4-(piperazin-1-ylmethyl)-2-propyl-3,4-dihydroisoquinolin-1(2<i>H</i>)-one (<i>trans</i>-<b>2</b>), which effectively suppressed Viruses502https://www.ebi.ac.uk/biostudies/studies/S-EPMC9965753biostudies-literatureNovel Tetrahydroisoquinoline-Based Heterocyclic Compounds Efficiently Inhibit SARS-CoV-2 Infection <i>In Vitro</i>.PMC9965753Wang MLi YLi JBurdzhiev NTLozanova VVHu HKandinska MIWang XfalseNovel Tetrahydroisoquinoline-Based Heterocyclic Compounds Efficiently Inhibit SARS-CoV-2 Infection <i>In Vitro</i>.The ongoing COVID-19 pandemic has caused over six million deaths and huge economic burdens worldwide. Antivirals against its causative agent, SARS-CoV-2, are in urgent demand. Previously, we reported that heterocylic compounds, i.e., chloroquine (CQ) and hydroxychloroquine (HCQ), are potent in inhibiting SARS-CoV-2 replication <i>in vitro</i>. In this study, we discussed the syntheses of two novel heterocylic compounds: <i>tert</i>-butyl <i>rel</i>-4-(((3<i>R</i>,4<i>S</i>)-3-(1<i>H</i>-indol-3-yl)-1-oxo-2-propyl-1,2,3,4-tetrahydroisoquinolin-4-yl)methyl)piperazine-1-carboxylate (<i>trans</i>-<b>1</b>) and <i>rel</i>-(3<i>R</i>,4<i>S</i>)-3-(1<i>H</i>-indol-3-yl)-4-(piperazin-1-ylmethyl)-2-propyl-3,4-dihydroisoquinolin-1(2<i>H</i>)-one (<i>trans</i>-<b>2</b>), which effectively suppressed 2023-01-01T00:00:00Z2023 Feb2025-04-22T20:58:42.366Z2025-04-06T03:25:15.017ZS-EPMC99657533685171610.3390/v15020502