New carboxyalkyl inhibitors of brain enkephalinase: synthesis, biological activity, and analgesic properties.

@article{FourniZaluski1983NewCI,
  title={New carboxyalkyl inhibitors of brain enkephalinase: synthesis, biological activity, and analgesic properties.},
  author={Marie-Claude Fourni{\'e}-Zaluski and Pascale Chaillet and E Soroca-Lucas and H Marçais-Collado and Jean Costentin and B. Roques},
  journal={Journal of medicinal chemistry},
  year={1983},
  volume={26 1},
  pages={60-5}
}
New carboxyalkyl compounds derived from Phe-Leu and Phe-Ala were synthesized and checked as inhibitors of "enkephalinase", a metalloendopeptidase cleaving the Gly3-Phe4 bond of enkephalins from mouse striatal membranes. Differential recognition of both brain enkephalinase and angiotensin-converting enzyme (ACE) catalytic sites by these carboxylalkyl compounds lead to potent (KI approximately 0.5 microM), competitive and selective inhibitors of the enkephalin-degrading enzyme. The most… CONTINUE READING