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Bioorg Med Chem Lett. 2008 Jan 15;18(2):460-3. Epub 2007 Dec 3.

Conformationally constrained diketopimelic acid analogues as inhibitors of dihydrodipicolinate synthase.

Author information

1
School of Chemistry, University of Melbourne, Vic. 3010, Australia.

Abstract

Dihydrodipicolinate synthase (DHDPS) is a key enzyme in lysine biosynthesis and a potential antibiotic target. The enzyme catalyses the condensation of (S)-aspartate semi-aldehyde (ASA) and pyruvate to form dihydrodipicolinate. Constrained diketopimelic acid derivatives have been designed as mimics of the acyclic enzyme-bound condensation product of ASA and pyruvate. Several of the compounds are shown to be active, slow-binding inhibitors with improved inhibition of DHDPS.

PMID:
18077163
DOI:
10.1016/j.bmcl.2007.11.108
[Indexed for MEDLINE]

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