1609973-52-5Relevant articles and documents
Design and synthesis of highly potent HIV-1 protease inhibitors with novel isosorbide-derived P2 ligands
Qiu, Xin,Zhao, Guo-Dong,Tang, Long-Qiang,Liu, Zhao-Peng
supporting information, p. 2465 - 2468 (2014/05/20)
The design, synthesis, and biological evaluation of a series of six HIV-1 protease inhibitors incorporating isosorbide moiety as novel P2 ligands are described. All the compounds are very potent HIV-1 protease inhibitors with IC50 values in the nanomolar or picomolar ranges (0.05-0.43 nM). Molecular docking studies revealed the formation of an extensive hydrogen-bonding network between the inhibitor and the active site. Particularly, the isosorbide-derived P2 ligand is involved in strong hydrogen bonding interactions with the backbone atoms.
