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HIV/AIDS Drug Development

Tricyclic HIV integrase inhibitor has increased potency and solubility

Published in AIDS Weekly, October 2nd, 2006

Tricyclic HIV integrase inhibitor has increased potency and solubility.

"A novel class of tricyclic 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," scientists in the United States report.

According to H.L. Jin and colleagues at Gilead Sciences Inc., "The efficient syntheses of pyrroloquinoline tricyclic analogs are described."

"The SAR studies resulted in the identification of a lead compound that is more potent and more soluble than L-870810," concluded...

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