Synthesis of (3R)-amino-(2S)-hydroxy amino acids for inhibition of methionine aminopeptidase-1

摘要

(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. [References: 15]