245741-47-3Relevant academic research and scientific papers
4-Hydroxy-5,6-dihydro-2H-pyran-2-ones. 3. Bicyclic and hetero-aromatic ring systems as 3-position scaffolds to bind to S1' and S1' of the HIV-1 protease enzyme
Ellsworth, Edmund L.,Domagala, John,Vara Prasad,Hagen, Susan,Ferguson, Donna,Holler, Tod,Hupe, Donald,Graham, Neil,Nouhan, Caroline,Tummino, Peter J.,Zeikus, Greg,Lunney, Elizabeth A.
, p. 2019 - 2024 (2007/10/03)
56-Dihydro-2H-pyran-2-ones are potent inhibitors of HIV-1 protease which bind to the S1 S2 S1' S2' pockets have a unique binding mode with the catalytic aspartyl groups the flap region of the enzyme. Efforts to explore 3-position heterocyclic scaffolds that bind to the S1' S2' pockets have provided a number of selected analogs that display high HIV-1 protease inhibitory activity.
