Difluoromethylene analogues of aspartyl phosphate: The first synthetic inhibitors of aspartate semi-aldehyde dehydrogenase

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Original languageEnglish
Pages (from-to)1710-1711
Number of pages2
JournalChemical communications
Volume1
Issue number18
Publication statusPublished - 1 Jan 2001
Externally publishedYes

Abstract

The difluoromethylene analogue of aspartyl phosphate 6 has been prepared by the fluoride catalysed coupling of diethyl trimethylsilyldifluoromethyl phosphonate with an appropriate aldehyde followed by Dess-Martin oxidation and deprotection; the deprotected compound inhibited (KI 95 μM) aspartate semi-aldehyde dehydrogenase, a key enzyme involved in bacterial amino acid and peptidoglycan biosynthesis.

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Difluoromethylene analogues of aspartyl phosphate: The first synthetic inhibitors of aspartate semi-aldehyde dehydrogenase. / Cox, Russell J.; Hadfield, Andrea T.; Mayo-Martín, M. Belén.
In: Chemical communications, Vol. 1, No. 18, 01.01.2001, p. 1710-1711.

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