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Verschueren, W.G. et al.

Verschueren, Dierynck, Amssoms, Hu, Boonants, Pille, Daeyaert, Hertogs, Surleraux, Wigerinck,

Design and optimization of tricyclic phtalimide analogues as novel inhibitors of HIV-1 integrase.

Human immunodeficiency virus type-1 integrase is an essential enzyme for effective viral replication and hence a valid target for the design of inhibitors. We report here on the design and synthesis of a novel series of phthalimide analogues as integrase inhibitors. The short synthetic pathway enabled us to synthesize a series of analogues with a defined structure diversity. The presence of a single carbonyl-hydroxy-aromatic nitrogen motif was shown to be essential for the enzymatic activity and this was confirmed by molecular docking studies. The enzymatically most active compound from this series is 7-(3,4-dichlorobenzyl)-5,9-dihydroxypyrrolo[3,4-g]quinoxaline-6,8-dione (15l) with an IC(50) value of 112 nM on the HIV-1 integrase enzyme, while ((7-(4-chlorobenzyl)-5,9-dihydroxy-pyrrolo[3,4-g]quinoxaline-6,8-dione (15k)) showed an EC(50) of 270 nM against HIV-1 in a cell-based assay.[1]

References

Design and optimization of tricyclic phtalimide analogues as novel inhibitors of HIV-1 integrase. Verschueren, W.G., Dierynck, I., Amssoms, K.I., Hu, L., Boonants, P.M., Pille, G.M., Daeyaert, F.F., Hertogs, K., Surleraux, D.L., Wigerinck, P.B. J. Med. Chem. (2005) [Pubmed]

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