Synthesis and in vitro enzyme activity of peptide derivatives of bacterial cell wall biosynthesis inhibitors

…, JA Schouten, RA Stentiford, KJ Wareing

Index: Cox, Russell J.; Jenkins, Helen; Schouten, James A.; Stentiford, Rosie A.; Wareing, Katrina J. Journal of the Chemical Society, Perkin Transactions 1, 2000 , # 13 p. 2023 - 2036

Full Text: HTML

Citation Number: 0

Abstract

The enzyme diaminopimelate aminotransferase (DAP-AT) is a good potential target for the design of novel antibacterial agents. We have synthesised a series of peptide hydrazines based on the structure of the natural substrate of DAP-AT. These compounds show varied inhibition properties in vitrovs. DAP-AT from E. coli as well as moderate antimicrobial activity vs. E. coli. Examination of the kinetics of inhibition reveals that hydrazine, as well as the ...