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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors.

A novel class of tri-cyclic HIV integrase inhibitors were designed based on conformational analysis of 1,6-naphthyridine carboxamide compound L-870810 and docking the designed inhibitor into the active site of our integrase enzyme model. The efficient syntheses of pyrroloquinoline tri-cyclic analogs are described. The SAR studies resulted in the identification of a lead compound that is more potent and more soluble than L-870810.[1]

References

  1. Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors. Jin, H., Cai, R.Z., Schacherer, L., Jabri, S., Tsiang, M., Fardis, M., Chen, X., Chen, J.M., Kim, C.U. Bioorg. Med. Chem. Lett. (2006) [Pubmed]
 
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