Article
Bicyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors.
Chemical biology & drug design - 1 Feb 2012
Zhao Xue Zhi, Maddali Kasthuraiah, Metifiot Mathieu, Smith Steven J, Vu B Christie, Marchand Christophe, Hughes Stephen H, Pommier Yves, Burke Terrence R
Abstract excerpt
HIV-1 integrase (IN) is a validated therapeutic target for the treatment of AIDS. However, the emergence of resistance to raltegravir, the sole marketed FDA-approved IN inhibitor, emphasizes the need to develop second-generation inhibitors that retain efficacy against clinically relevant IN mutants. We report herein bicyclic hydroxy-1H-pyrrolopyridine-triones as a new family of HIV-1 integrase inhibitors that...
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