A series of stereochemically defined cyclic ethers as P2-ligands were incorporated in an allophenylnorstatine-based isostere to provide a new series of HIV-1 protease inhibitors. Inhibitors 3b and 3c, containing conformationally constrained cyclic ethers, displayed impressive enzymatic and antiviral properties and represent promising lead compounds for further optimization. © 2009 Elsevier Ltd.
Ghosh, A.K., Gemma, S., Simoni, E., Baldridge, A., Walters, D.E., Ide, K., et al. (2010). Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 20(3), 1241-1246 [10.1016/j.bmcl.2009.11.123].
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands
Gemma, Sandra;
2010-01-01
Abstract
A series of stereochemically defined cyclic ethers as P2-ligands were incorporated in an allophenylnorstatine-based isostere to provide a new series of HIV-1 protease inhibitors. Inhibitors 3b and 3c, containing conformationally constrained cyclic ethers, displayed impressive enzymatic and antiviral properties and represent promising lead compounds for further optimization. © 2009 Elsevier Ltd.
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https://hdl.handle.net/11365/11876
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