1H-Pyrrole-2-carboxamide, N-[(1S)-2-amino-1-[4-(hydroxymethyl)-2-thiazolyl]ethyl]-5-[3-fluoro-4-(trifluoromethyl)phenyl]-

Description

NBD-14189 is a potent HIV-1 entry antagonist with an IC₅₀ of 89 nM against the HIV-1_HXB2 pseudovirus. NBD-14189 binds to HIV-1 gp120 and shows potent antiviral activity (EC₅₀<200 nM)^[1][2].

NBD-14189 has anti-HIV-1 activity (IC₅₀=0.089 μM) and cytotoxicity (CC₅₀=21.9 μM) in single-cycle (TZM-bl cells) assays. NBD-14189 has anti-HIV-1 activity (IC₅₀=0.18 μM) and cytotoxicity (CC₅₀=22.1 μM) in multi-cycle (MT-2 cells) assays^[1].
NBD-14189 (0-50 μM) prevents HIV-1 mediated cell-cell fusion with an IC₅₀ of 9.4 μM in indicator cells TZM-bl cells were cocultured with Env- and Tat-expressing HL2/3 cells^[1].
NBD-14189 shows weak or no inhibition of the hERG current, with an IC₅₀ of 3.0 μM, respectively^[1].

Uses

NBD-14189 is a potent HIV-1 entry antagonist with an IC50of 89 nM against the HIV-1HXB2pseudovirus. NBD-14189 binds to HIV-1 gp120 and shows potent antiviral activity (EC50<200 nM)[1][2].

IC 50

HIV-1

References

[1] Francesca Curreli, et al. Structure-based lead optimization to improve antiviral potency and ADMET properties of phenyl-1H-pyrrole-carboxamide entry inhibitors targeted to HIV-1 gp120. Eur J Med Chem. 2018 Jun 25;154:367-391. DOI:10.1016/j.ejmech.2018.04.062
[2] Natalie Losada, et al. HIV-1 gp120 Antagonists Also Inhibit HIV-1 Reverse Transcriptase by Bridging the NNRTI and NRTI Sites. J Med Chem. 2021 Nov 25;64(22):16530-16540. DOI:10.1021/acs.jmedchem.1c01104