Synthesis and structure-activity relations of bestatin analogs, inhibitors of aminopeptidase B

R Nishizawa, T Saino, T Takita, H Suda…

Index: Takita,T. et al. Journal of Medicinal Chemistry, 1977 , vol. 20, p. 510 - 515

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Citation Number: 171

Abstract

Stereoisomers and analogues of bestatin,[(2S, 3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-~- leucine, were synthesized and tested for aminopeptidase B and leucine aminopeptidase inhibiting activity. Among the eight stereoisomers, the 2s stereoisomers exhibited strong activity. In a series of compounds in which the L-leucine residue of bestatin was substituted with other amino acids, only the one containing isoleucine showed more activity than ...