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Type: Journal article
Title: Rational Design, Synthesis, and Evaluation of Nanomolar Type II Dehydroquinase Inhibitors
Author: Payne, R.
Peyrot, F.
Kerbarh, O.
Abell, A.
Abell, C.
Citation: ChemMedChem, 2007; 2(7):1015-1029
Publisher: Wiley - V C H Verlag GmbH & Co. KGaA
Issue Date: 2007
ISSN: 1860-7179
Abstract: The in silico design, synthesis, and biological evaluation of ten potent type II dehydroquinase inhibitors are described. These compounds contain an anhydroquinate core, incorporated as a mimic of the enolate reaction intermediate. This substructure is attached by a variety of linking units to a terminal phenyl group that binds in an adjacent pocket. Inhibitors were synthesised from (-)-quinic acid using palladium-catalysed Stille and carboamidation chemistry. Several inhibitors exhibited nanomolar inhibition constants against type II dehydroquinases from Streptomyces coelicolor and Mycobacterium tuberculosis. These are among the most potent inhibitors of these enzymes reported to date.
Keywords: Antimicrobials; cross-coupling; dehydroquinase; inhibitors; tuberculosis
RMID: 0020084714
DOI: 10.1002/cmdc.200700032
Appears in Collections:Chemistry and Physics publications

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