Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10592119 | Bioorganic & Medicinal Chemistry Letters | 2014 | 4 Pages |
Abstract
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 (0.05-0.43Â 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.
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Authors
Xin Qiu, Guo-Dong Zhao, Long-Qiang Tang, Zhao-Peng Liu,