Document 0550
 DOCN  M9590550
 TI    Alpha-ketoamide Phe-Pro isostere as a new core structure for the
       inhibition of HIV protease.
 DT    9509
 AU    Munoz B; Giam CZ; Wong CH; Department of Chemistry, Scripps Research
       Institute, La Jolla, CA; 92037, USA.
 SO    Bioorg Med Chem. 1994 Oct;2(10):1085-90. Unique Identifier : AIDSLINE
       MED/95291690
 AB    Studies on the inhibition of HIV-1 protease utilizing a core isostere
       with replacement of the scissle bond for an alpha-amino-ketone have
       resulted in the development of an alpha-keto-amide isosteric replacement
       of the Phe-Pro scissle amide bond. The simple dipeptide isostere was
       shown to be a promising new core structure for the development of the
       enzyme inhibitors. The Ki of this core structure was determined to be 6
       microM, compared to 230 microM and > 50 microM for the corresponding
       phosphinic acid and hydroxyethylamine isosteres.
 DE    Amides/CHEMISTRY/PHARMACOLOGY  Amines/CHEMISTRY/PHARMACOLOGY  Amino Acid
       Sequence  Dipeptides/*CHEMISTRY/PHARMACOLOGY  Escherichia coli  HIV
       Protease Inhibitors/*CHEMISTRY/PHARMACOLOGY
       Ketones/CHEMISTRY/PHARMACOLOGY  Kinetics  Molecular Sequence Data
       Phenylalanine/CHEMISTRY  Proline/CHEMISTRY  Recombinant Fusion
       Proteins/ANTAGONISTS & INHIB  Support, U.S. Gov't, P.H.S.  JOURNAL
       ARTICLE

       SOURCE: National Library of Medicine.  NOTICE: This material may be
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