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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

โœ 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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โœฆ 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.;


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Small dipeptide-based HIV protease inhib
โœ Yoshiaki Kiso; Hikaru Matsumoto; Sota Mizumoto; Tooru Kimura; Yoichi Fujiwara; K ๐Ÿ“‚ Article ๐Ÿ“… 1999 ๐Ÿ› Wiley (John Wiley & Sons) ๐ŸŒ English โš– 312 KB

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