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Chemical Compound Review:

Palinavir N-[(1S)-1-[[(2S,3R)-3- hydroxy-1-phenyl-4...

Synonyms: SureCN6796, BILA-2011, CHEMBL13134, BILA-2011-BS, AC1Q5FYE, ...

Lamarre, D. et al., Beaulieu, P.L. et al., Ohlmann, T. et al.

Ohlmann, Prévôt, Décimo, Roux, Garin, Morley, Darlix, Beaulieu, Anderson, Cameron, Croteau, Gorys, Grand-Maître, Lamarre, Liard, Paris, Plamondon, Soucy, Thibeault, Wernic, Yoakim, Pav, Tong,

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Disease relevance of BILA-2011

Our results show that eIF4GI, but not eIF4GII, is substrate for HIV-1 protease and this effect can be prevented by a HIV-1 protease inhibitor, palinavir [1].
Starting from palinavir (1), our lead HIV protease inhibitor, we have discovered a new series of truncated analogues in which the P(3)-P(2) quinaldic-valine portion of 1 was replaced by 2', 6'-dimethylphenoxyacetyl [2].
Palinavir is a potent inhibitor of the human immunodeficiency virus type 1 (HIV-1) and type 2 (HIV-2) proteases [3].
Replication of laboratory strains (HIV-1, HIV-2, and simian immunodeficiency virus) and HIV-1 clinical isolates is inhibited by palinavir with 50% effective concentrations ranging from 0.5 to 30 nM [3].

High impact information on BILA-2011

Palinavir retains anti-HIV-1 activity when administered postinfection until times subsequent to the reverse transcription step [3].

References

In vitro cleavage of eIF4GI but not eIF4GII by HIV-1 protease and its effects on translation in the rabbit reticulocyte lysate system. Ohlmann, T., Prévôt, D., Décimo, D., Roux, F., Garin, J., Morley, S.J., Darlix, J.L. J. Mol. Biol. (2002) [Pubmed]
2',6'-Dimethylphenoxyacetyl: a new achiral high affinity P(3)-P(2) ligand for peptidomimetic-based HIV protease inhibitors. Beaulieu, P.L., Anderson, P.C., Cameron, D.R., Croteau, G., Gorys, V., Grand-Maître, C., Lamarre, D., Liard, F., Paris, W., Plamondon, L., Soucy, F., Thibeault, D., Wernic, D., Yoakim, C., Pav, S., Tong, L. J. Med. Chem. (2000) [Pubmed]
Antiviral properties of palinavir, a potent inhibitor of the human immunodeficiency virus type 1 protease. Lamarre, D., Croteau, G., Wardrop, E., Bourgon, L., Thibeault, D., Clouette, C., Vaillancourt, M., Cohen, E., Pargellis, C., Yoakim, C., Anderson, P.C. Antimicrob. Agents Chemother. (1997) [Pubmed]

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