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

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Ksander GM, Diefenbacher CG, Yuan AM, Clark F, Sakane Y, Ghai RD

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

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

PubMed ID

2585440 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Phosphoramidon	Neprilysin	IC 50 (nM)	0.4	N/A	N/A	Details
Thiorphan	Neprilysin	IC 50 (nM)	5	N/A	N/A	Details