Novel HIV-1 protease inhibitors have been prepared in a enantioselective manner via an Evans asymmetric aldol, Claisen rearrangement and icdolactonization. X-ray crystallographic analysis was used to confirm the absolute configuration of the newly created stereogenic centers. The alarming spread of
A Concise Synthesis of Silanediol-Based Transition-State Isostere Inhibitors of Proteases
โ Scribed by Organ, Michael G.; Buon, Christophe; Decicco, Carl P.; Combs, Andrew P.
- Book ID
- 120262324
- Publisher
- American Chemical Society
- Year
- 2002
- Tongue
- English
- Weight
- 37 KB
- Volume
- 4
- Category
- Article
- ISSN
- 1523-7060
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๐ SIMILAR VOLUMES
A series of 1,3-diamino-2-propanol derivatives have been synthesized on solid phase as potential aspar'tic acid protease irdaibitors. The developed methodology allows the incorporation of either an alkyl group or H at the R 2 site of hydroxyethylamine isostere.
## Peptidomimetic Human The human immunodeficiency virus (HIV) codas f o r an u.spartic protease known to be essential $)r retroviral mat urution and replicution. The H I V proteuw can rmignize Phe-Pro and Tyr-Pro sequences as the virus-specific cleuvuge site. These.fi.atures provided a basisJor th