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

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

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

doi

10.1021/jm00132a005

subject

Has Abstract

pub_date

1989-12-01 00:00:00

pages

2519-26

issue

12

eissn

0022-2623

issn

1520-4804

journal_volume

32

pub_type

杂志文章

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