Uses
NBD-556 is a N-phenyl-N'-(2,2,6,6-tetramethyl-piperidin-4-yl)-oxalamide analog, a novel class of human immunodeficiency virus type 1 (HIV-1) entry inhibitors that block the gp120-CD4 interaction.
Biological Activity
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].
IC 50
nbd-556 inhibited cell–cell fusion between h9/hiv-1iiib and mt-2 (ic50 ~3 μm)
References
[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.
