期刊
BIOCHEMICAL SOCIETY TRANSACTIONS
卷 33, 期 -, 页码 772-775出版社
PORTLAND PRESS LTD
DOI: 10.1042/BST0330772
关键词
deazathiamine diphosphate (deazaTPP); Friedel-Crafts acylation reaction; thiazolium ring; V-conformation; ylid
The 3-deaza analogue of TPP (thiamine diphosphate), a close mimic of the ylid intermediate, has been synthesized and is an extremely potent inhibitor of a variety of TPP-dependent enzymes, binding much more tightly than TPP itself. Results using deazaTPP complexed with the El subunit of PDH (pyruvate dehydrogenase) have led to a novel proposal about the mechanism of this enzyme. The 2-substituted forms of deazaTPP, which mimic other intermediates in the catalytic mechanism, can also be synthesized and 2-(1-hydroxyethyl)deazaTPP is also an extremely potent inhibitor of PDC (pyruvate decarboxylase). Attachment of such 2-substituents is expected to be a way to introduce selectivity in the inhibition of various TPP-dependent enzymes.
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