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J Med Chem. 1989 Dec;32(12):2519-26.

Enkephalinase inhibitors. 1. 2,4-Dibenzylglutaric acid derivatives.

Author information

1
Research Department, CIBA-GEIGY Corporation, Summit, New Jersey 07901.

Abstract

The synthesis of two new series of dicarboxylic acid dipeptides and two sulfhydryl-containing inhibitors are described. The in vitro enkephalinase inhibition data and some in vivo analgesic data are presented for these compounds. For the dibenzylglutaric acid series structure-activity relationships and in vivo analgesic activity are discussed. The reverse amides, i.e., 4-amino-2,4-dibenzylbutyric acid derivatives, are also discussed. Two sulfhydryl-containing inhibitors showed good in vivo potency in the mouse jump-latency hot-plate test after peripheral administration at moderate low doses.

PMID:
2585440
DOI:
10.1021/jm00132a005
[Indexed for MEDLINE]

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