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Lysine sulfonamides as novel HIV-Protease inhibitors: optimization of theNε-acyl-phenyl spacer

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
13
Issue
24
Identifiers
DOI: 10.1016/j.bmcl.2003.09.058
Disciplines
  • Biology

Abstract

Abstract A series of Nα-isobutyl- Nα-arylsulfonamido-( Nε acyl) lysine and lysinol derivatives were prepared and evaluated as inhibitors of HIV protease and wild type virus. A simple original synthesis was devised to form Nα-(arylsulfonamide)- Nα-isobutyl lysine, which could be easily acylated with carboxylic acids at the Nε position. A two-atom spacer was found to be optimal between this acyl group and a phenyl yielding compounds of sub-nanomolar potency on purified enzyme.

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