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

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

Index: Jeon, Heung-Bae; Lee, Younghee; Qiao, Chunhua; Huang, He; Sayre, Lawrence M. Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 21 p. 4631 - 4641

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Citation Number: 29

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 μM. 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 ...