First hydroxamate inhibitors for carboxypeptidase A. N-acyl-N-hydroxy-beta-phenylalanines

Bioorg Med Chem Lett. 1999 Mar 8;9(5):691-6. doi: 10.1016/s0960-894x(99)00055-4.

Abstract

A series of N-acyl-N-hydroxy-beta-Phe were designed, synthesized, and shown to have potent inhibitory activity for carboxypeptidase A (CPA). They are the first examples of CPA inhibitors having a hydroxamate functionality.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bacillus / enzymology
  • Carboxypeptidases / antagonists & inhibitors*
  • Carboxypeptidases / chemistry
  • Carboxypeptidases A
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Phenylalanine / chemical synthesis*
  • Phenylalanine / pharmacology
  • Protein Conformation
  • Structure-Activity Relationship
  • Thermolysin / antagonists & inhibitors
  • Thermolysin / chemistry
  • Thermolysin / metabolism

Substances

  • Enzyme Inhibitors
  • Phenylalanine
  • Carboxypeptidases
  • Carboxypeptidases A
  • Thermolysin