Design and synthesis of stereochemically defined novel spirocyclic P2-ligands for HIV-1 protease inhibitors |
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Authors: | Ghosh Arun K Chapsal Bruno D Baldridge Abigail Ide Kazuhiko Koh Yashiro Mitsuya Hiroaki |
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Institution: | Departments of Chemistry and Medicinal Chemistry, Purdue University, West Lafayette, Indiana 47907, USA. akghosh@purdue.edu |
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Abstract: | The synthesis of a series of stereochemically defined spirocyclic compounds and their use as novel P2-ligands for HIV-1 protease inhibitors are described. The bicyclic core of the ligands was synthesized by an efficient nBu 3SnH-promoted radical cyclization of a 1,6-enyne followed by oxidative cleavage. Structure-based design, synthesis of ligands, and biological evaluations of the resulting inhibitors are reported. |
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