Synthesis and structure-activity relationships of amastatin analogues, inhibitors of aminopeptidase A

H Tobe, H Morishima, T Aoyagi…

Index: Tobe; Morishima; Aoyagi; et al. Agricultural and Biological Chemistry, 1982 , vol. 46, # 7 p. 1865 - 1872

Full Text: HTML

Citation Number: 23

Abstract

Stereoisomers and analogues of amastatin,[(2 S, 3 R)-3-amino-2-hydroxy-5- methylhexanoyl]-l-Val-l-Val-l-Asp, were synthesized and their inhibitory activities towards aminopeptidase A (AP-A) and other arylamidases tested. Among the four stereoisomers of a new amino acid residue in amastatin, the 2 S stereoisomers exhibited strong activity. In a series of compounds in which the C-terminal amino acid of amastatin was substituted by ...