ChemInform Abstract: KNI-577, a Potent Small-Sized HIV Protease Inhibitor Based on the Dipeptide Containing the Hydroxymethylcarbonyl Isostere as an Ideal Transition-State Mimic
โ Scribed by Y. KISO; S. YAMAGUCHI; H. MATSUMOTO; T. MIMOTO; R. KATO; S. NOJIMA; H. TAKAKU; T. FUKAZAWA; T. KIMURA; K. AKAJI
- Publisher
- John Wiley and Sons
- Year
- 2010
- Weight
- 29 KB
- Volume
- 29
- Category
- Article
- ISSN
- 0931-7597
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โฆ Synopsis
KNI-577, a Potent Small-Sized HIV Protease Inhibitor Based on the Dipeptide Containing the Hydroxymethylcarbonyl Isostere as an Ideal Transition-State Mimic -[synthesis of the title compound (I), which exhibits potent antiviral activities, low cytotoxicity and good pharmacokinetic properties after intraduodenal administration]. -(KISO, Y.;
๐ SIMILAR VOLUMES
The human immunodeficiency virus (HIV) codes for an aspartic protease known to be essential for retroviral maturation and replication. HIV protease is formed from two identical 99 amino acid peptides. We synthesized [(NHCH 2 CH 2 -S-CH 2 CO) [51][52] , Ala 67,95 ]HIV-1 protease using the thioether c