Bioorganic & medicinal chemistry

3-Amino-2-hydroxy-propionaldehyde and 3-amino-1-hydroxypropan-2-one derivatives: New classes of aminopeptidase inhibitors

C Tarnus, JM Rémy, H d'Orchymont

文献索引：Tarnus, Celine; Remy, Jean-Marc; D'Orchymont, Hugues Bioorganic and Medicinal Chemistry, 1996 , vol. 4, # 8 p. 1287 - 1297

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被引用次数: 9

摘要

3-Amino-2-hydroxy-propionaldehydes [H2NCH (R) CHOHCHO with R= H, i-Bu, CH2Ph] were designed as metalloaminopeptidase inhibitors based on the metal active site chelation concept. These compounds were found to be micromolar inhibitors of aminopeptidase-M (AP-M, EC 3.4. 11.2) with potencies similar to bestatin (Ki= 3.5 μM). Notably, compound 5a (R= H) is a selective inhibitor of AP-M (Ki= 7 μM) with respect to cytosolic leucine ...