Synthesis and in vitro enzyme activity of an oxa analogue of azi-DAP

被引：15

作者：

Cox, RJ

Durston, J

Roper, DI

机构：

[1] Univ Bristol, Sch Chem, Bristol BS8 1TS, Avon, England

[2] Univ Warwick, Dept Biol Sci, Coventry CV4 7AL, W Midlands, England

来源：

JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1 | 2002年 / 08期

关键词：

D O I：

10.1039/b201727j

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The synthesis of a novel epoxide inhibitor 6 of meso-DAP epimerase was achieved. A new and convenient assay for meso-DAP epimerase was devised which is a considerable improvement on previously reported assay methods. This assay was used to determine the inhibitory properties of 6. The epoxide 6 shows limited competitive inhibition vs. meso-DAP epimerase, but clear time dependent inhibition indicative of the expected covalent attachment at the active site. Epoxide 6, although an effective inhibitor of meso-DAP epimerase, was unstable at pH 7.3 in aqueous buffer, being hydrolysed to the corresponding diol.

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页码：1029 / 1035

页数：7

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