6, 7-Dihydroxy-1-oxoisoindoline-4-sulfonamide-containing HIV-1 integrase inhibitors

…, BC Johnson, C Marchand, SH Hughes…

Index: Zhao, Xue Zhi; Maddali, Kasthuraiah; Smith, Steven J.; Metifiot, Mathieu; Johnson, Barry C.; Marchand, Christophe; Hughes, Stephen H.; Pommier, Yves; Burke Jr., Terrence R. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 24 p. 7309 - 7313

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Citation Number: 14

Abstract

Although an extensive body of scientific and patent literature exists describing the development of HIV-1 integrase (IN) inhibitors, Merck's raltegravir and Gilead's elvitegravir remain the only IN inhibitors FDA-approved for the treatment of AIDS. The emergence of raltegravir-resistant strains of HIV-1 containing mutated forms of IN underlies the need for continued efforts to enhance the efficacy of IN inhibitors against resistant mutants. We ...