Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection

…, C Gardelli, O Gonzalez Paz, DJ Hazuda…

文献索引：Summa, Vincenzo; Petrocchi, Alessia; Bonelli, Fabio; Crescenzi, Benedetta; Donghi, Monica; Ferrara, Marco; Fiore, Fabrizio; Gardelli, Cristina; Paz, Odalys Gonzalez; Hazuda, Daria J.; Jones, Philip; Kinzel, Olaf; Laufer, Ralph; Monteagudo, Edith; Muraglia, Ester; Nizi, Emanuela; Orvieto, Federica; Pace, Paola; Pescatore, Giovanna; Scarpelli, Rita; Stillmock, Kara; Witmer, Marc V.; Rowley, Michael Journal of Medicinal Chemistry, 2008 , vol. 51, # 18 p. 5843 - 5855

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被引用次数: 425

摘要

Human immunodeficiency virus type-1 (HIV-1) integrase is one of the three virally encoded enzymes required for replication and therefore a rational target for chemotherapeutic intervention in the treatment of HIV-1 infection. We report here the discovery of Raltegravir, the first HIV-integrase inhibitor approved by FDA for the treatment of HIV infection. It derives from the evolution of 5, 6-dihydroxypyrimidine-4-carboxamides and N-methyl-4- ...