Work

Design and Synthesis of Stereochemically Defined Novel Spirocyclic P2-Ligands for HIV-1 Protease Inhibitors

Year: 2008

Type: article

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.

Source: Organic Letters

DOI: 10.1021/ol8020308

Authors: Arun K. Ghosh, Bruno D. Chapsal, Abigail Baldridge, Kazuhiko Ide, Yashiro Koh, Hiroaki Mitsuya

Institutions: Purdue University West Lafayette, National Cancer Institute, Center for Cancer Research, Kumamoto University

Language: English

Topic: HIV/AIDS drug development and treatment

Subfield: Infectious Diseases

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: green

Funders: National Institutes of Health, National Institute of General Medical Sciences