L-Tyrosine, N-[[8-(cyclohexyloxy)-1-oxo-2-phenyl-1H-pyrido[2,1-b]benzothiazol-4-yl]carbonyl]-

Biological Activity

HeE1-2Tyr, a pyridobenzothiazole compound, is a flavivirus RNA dependent RNA polymerases (RdRp) inhibitor. HeE1-2Tyr significantly inhibits West Nile, Dengue and SARS-CoV-2 RdRps (IC50 of 27.6 μM) activity in vitro[1][2]. HeE1-2Tyr shows antiviral activity, it is able to inhibit an Ugandan strain of West Nile virus with an IC50 of 2.1 μM, as well as all the four Dengue virus (DENV) serotypes, with IC50 ranging from 6.8 to 15 μM. The cytotoxicity of HeE1-2Tyr versus Vero E6 cells is ~115 μM[1].Additionally, upon infection of human HEK 293 cells (CC50 of 50 μM), HeE1-2Tyr inhibits clinical strains of yellow fever virus with IC50 values ranging from 3.9 to 12 μM[1]. HeE1-2Tyr completely inhibits the replication of both SARS-CoV-2 and Feline coronavirus (FIPV)[2].

References

[1]. Delia Tarantino, et al. Targeting flavivirus RNA dependent RNA polymerase through a pyridobenzothiazole inhibitor. Antiviral Res. 2016 Oct;134:226-235. [2]. Milan Dejmek, et al. Non-Nucleotide RNA-Dependent RNA Polymerase Inhibitor That Blocks SARS-CoV-2 Replication. Viruses. 2021 Aug 11;13(8):1585.