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Inhibition of bovine plasma amine oxidase by 1,4-diamino-2-butenes and -2-butynes.

Abstract：

:Bovine plasma amine oxidase (BPAO) was previously shown to be irreversibly inhibited by propargylamine and 2-chloroallylamine. 1,4-Diamine versions of these two compounds are here shown to be highly potent inactivators, with IC50 values near 20 microM. Mono-N-alkylation or N,N-dialkylation greatly lowered the inactivation potency in every case, whereas the mono-N-acyl derivatives were also weaker inhibitors and enzyme activity was recoverable. The finding that the bis-primary amines 1,4-diamino-2-butyne (a known potent inhibitor of diamine oxidases) and Z-2-chloro-1,4-diamino-2-butene are potent inactivators of BPAO is suggestive of unexpected similarities between plasma amine oxidase and the diamine oxidases and implies that it may be unwise to attempt to develop selective inhibitors of diamine oxidase using a diamine construct.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Jeon HB,Lee Y,Qiao C,Huang H,Sayre LM

doi

10.1016/s0968-0896(03)00521-2

subject

Has Abstract

pub_date

2003-10-15 00:00:00

pages

4631-41

issue

21

eissn

0968-0896

issn

1464-3391

pii

S0968089603005212

journal_volume

11

pub_type

杂志文章

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