Difluoromethylene analogues of aspartyl phosphate: the first synthetic inhibitors of aspartate semi-aldehyde dehydrogenase |
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| Authors: | Cox R J Hadfield A T Mayo-Martín M B |
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| Affiliation: | School of Chemistry, University of Bristol, Cantock's Close, Bristol BS8 1TS, UK. r.j.cox@bris.ac.uk |
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| 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 microM) aspartate semi-aldehyde dehydrogenase, a key enzyme involved in bacterial amino acid and peptidoglycan biosynthesis. |
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