1048979-59-4Relevant academic research and scientific papers
Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase
Sweeney, Zachary K.,Dunn, James P.,Li, Yu,Heilek, Gabrielle,Dunten, Pete,Elworthy, Todd R.,Han, Xiaochun,Harris, Seth F.,Hirschfeld, Donald R.,Hogg, J. Heather,Huber, Walter,Kaiser, Ann C.,Kertesz, Denis J.,Kim, Woongki,Mirzadegan, Taraneh,Roepel, Michael G.,Saito, Y. David,Silva, Tania M.P.C.,Swallow, Steven,Tracy, Jahari L.,Villasenor, Armando,Vora, Harit,Zhou, Amy S.,Klumpp, Klaus
scheme or table, p. 4352 - 4354 (2009/04/07)
A series of benzyl pyridazinones were evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Several members of this series showed good activity against the wild-type virus and NNRTI-resistant viruses. The binding of inhibitor 5a to HIV-RT was analyzed by surface plasmon resonance spectroscopy. Pharmacokinetic studies of 5a in rat and dog demonstrated that this compound has good oral bioavailability in animal species. The crystal structure of a complex between HIV-RT and inhibitor 4c is also described.
