IC50: NBD-556 inhibited cell–cell fusion between H9/HIV-1IIIB and MT-2 (IC50 ~3 μM)
The entry of HIV-1 into host cells is mediated by the binding of the surface subunit gp120 to the host cell receptor CD4. NBD-556 is a novel class of human immunodeficiency virus type 1 (HIV-1) entry inhibitor that block the gp120–CD4 interaction with drug-like properties.
In vitro: A systematic study showed that NBD-556 and NBD-557 target viral entry by inhibiting the binding of HIV-1 envelope glycoprotein gp120 to the cellular receptor CD4 but did not inhibit reverse transcriptase, protease, or integrase, demonstrating that they do not target the later stages of the HIV-1 life cycle to inhibit HIV-1 infection. NBD-556 and NBD-557 were also active against HIV-1 laboratory-adapted strains including an AZT-resistant strain and HIV-1 primary isolates, showing that these compounds can potentially be further modified to become potent HIV-1 entry inhibitors [1].
In vivo: No animal in-vivo data available currently.
Clinical trial: No clinical data are available.
Reference:
[1] Zhao, Q. , L. Ma, S. Jiang, H. Lu, S. Liu, Y. He, N. Strick, N. Neamati, and A. K. Debnath. 2005. Identification of N-phenyl-N′-(2,2,6,6-tetramethyl-piperidin-4-yl)-oxalamides as a new class of HIV-1 entry inhibitors that prevent gp120 binding to CD4. Virology 339:213-225.