Synthesis and structure-activity relationships of bestatin analogues, inhibitors of aminopeptidase B.

@article{Nishizawa1977SynthesisAS,
  title={Synthesis and structure-activity relationships of bestatin analogues, inhibitors of aminopeptidase B.},
  author={R Nishizawa and T Saino and Teisuke Takita and Hiroyuki Suda and Takaaki Aoyagi},
  journal={Journal of medicinal chemistry},
  year={1977},
  volume={20 4},
  pages={510-5}
}
Stereoisomers and analogues of bestatin, [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-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 bestatin. Norleucine, norvaline, methionine, valine… CONTINUE READING