Journal of medicinal chemistry

Synthesis of sulfur-containing analogs of bestatin. Inhibition of aminopeptidases by. alpha.-thiolbestatin analogs

TD Ocain, DH Rich

文献索引：Ocain, Timothy D.; Rich, Daniel H. Journal of Medicinal Chemistry, 1988 ,  vol. 31,  # 11  p. 2193 - 2199

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被引用次数: 61

摘要

Sulfur-containing amino acid and peptide analogues of bestatin [((2S, 3R)-3-amino-2- hydroxy-4-phenyl-butanoy1)-L-leucine](1) have been synthesized and evaluated as inhibitors of aminopeptidase M (AP-M), leucine aminopeptidase (LAP), and aminopeptidase B (AP-B). The 2-thiolbestatin analogue (6) was found to be a potent inhibitor of all three aminopeptidases (AP-M, Ki= 4.4 pM; LAP, Ki= 0.55 pM; AP-B, Ki= 4.6 nM) but only a ...