Abstract
The synthesis of a new class of peptidomimetics 1a-j, based on a 1,4-benzodiazepine scaffold and on a C-terminal aspartyl aldehyde building block, is described. Compounds 1a-j provided significant inhibitory activity against falcipains 2A and 2B (FP-2A and FP-2B), two cysteine proteases from Plasmodium falciparum.
Publication types
-
Research Support, N.I.H., Extramural
MeSH terms
-
Animals
-
Antimalarials / chemical synthesis*
-
Antimalarials / chemistry
-
Aspartic Acid / analogs & derivatives*
-
Aspartic Acid / chemistry
-
Benzodiazepines / chemical synthesis*
-
Benzodiazepines / chemistry
-
Cysteine Endopeptidases / chemistry
-
Cysteine Proteinase Inhibitors / chemical synthesis*
-
Cysteine Proteinase Inhibitors / chemistry
-
Molecular Mimicry
-
Peptides / chemistry*
-
Plasmodium falciparum / enzymology
-
Structure-Activity Relationship
Substances
-
Antimalarials
-
Cysteine Proteinase Inhibitors
-
Peptides
-
Benzodiazepines
-
Aspartic Acid
-
aspartic semialdehyde
-
Cysteine Endopeptidases
-
falcipain 2