Synthesis of (3R)-Amino-(2S)-Hydroxy Amino Acids for Inhibition of Methionine Aminopeptidase-1

Abstract
(3R)-amino-(2S)-hydroxy heptanoic acid (AHHpA) was synthesized via asymmetric aminohydroxylation and coupled with di-and tripeptides to form three compounds that inhibit MetAP-1 with IC50 values in the low micromolar range.