Abstract
A method utilizing the strategy of epoxide opening by amine with water as co-solvent and screening in situ was developed for rapid discovery of protein inhibitors. Using this approach, HIV protease inhibitors with novel P1′ residues were identified in our study. This strategy should be applicable for the efficient assembly of diverse compound collections for inhibitors' discovery and optimization in other systems.
Original language | English |
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Pages (from-to) | 1058-1062 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 14 |
Issue number | 4 |
DOIs | |
State | Published - 15 Feb 2006 |
Externally published | Yes |
Keywords
- Epoxide opening
- HIV protease inhibitors
- In situ screening
- In water
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry