Design of Annulated Pyrazoles as Inhibitors of HIV-1 Reverse Transcriptase∥

…, JJ Kennedy-Smith, T Mirzadegan…

文献索引：Sweeney, Zachary K.; Harris, Seth F.; Arora, Nidhi; Javanbakht, Hassan; Li, Yu; Fretland, Jennifer; Davidson, James P.; Billedeau, J. Roland; Gleason, Shelley K.; Hirschfeld, Donald; Kennedy-Smith, Joshua J.; Mirzadegan, Taraneh; Roetz, Ralf; Smith, Mark; Sperry, Sarah; Suh, Judy M.; Wu, Jeffrey; Tsing, Stan; Villasenor, Armando G.; Paul, Amber; Su, Guoping; Heilek, Gabrielle; Hang, Julie Q.; Zhou, Amy S.; Jernelius, Jesper A.; Zang, Fang-Jie; Klumpp, Klaus Journal of Medicinal Chemistry, 2008 , vol. 51, # 23 p. 7449 - 7458

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被引用次数: 65

摘要

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are recommended components of preferred combination antiretroviral therapies used for the treatment of HIV. These regimens are extremely effective in suppressing virus replication. Structure-based optimization of diaryl ether inhibitors led to the discovery of a new series of pyrazolo [3, 4-c] pyridazine NNRTIs that bind the reverse transcriptase enzyme of human immunodeficiency virus-1 ( ...