Article
4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.
Journal of medicinal chemistry - 26 Jun 2014
Zhao Xue Zhi, Smith Steven J, Métifiot Mathieu, Marchand Christophe, Boyer Paul L, Pommier Yves, Hughes Stephen H, Burke Terrence R
Abstract excerpt
There are currently three HIV-1 integrase (IN) strand transfer inhibitors (INSTIs) approved by the FDA for the treatment of AIDS. However, the emergence of drug-resistant mutants emphasizes the need to develop additional agents that have improved efficacies against the existent resistant mutants. As reported herein, we modified our recently disclosed 1-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamides IN...
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