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Issue 15, 2010
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Inhibition of chorismate-utilising enzymes by 2-amino-4-carboxypyridine and 4-carboxypyridone and 5-carboxypyridone analogues

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Abstract

Several 2-amino-4-carboxypyridine, 4- and 5-carboxypyridone-based compounds were prepared and tested against three members of the chorismate-utilising enzyme family, anthranilate synthase, isochorismate synthase and salicylate synthase. Most compounds exhibited low micromolar inhibition of these three enzymes. The most potent inhibitor was a 4-carboxypyridone analogue bearing a lactate side chain on the pyridyl nitrogen which exhibited inhibition constants of 5, 91 and 54 μM against anthranilate synthase, isochorismate synthase and salicylate synthase respectively.

Graphical abstract: Inhibition of chorismate-utilising enzymes by 2-amino-4-carboxypyridine and 4-carboxypyridone and 5-carboxypyridone analogues

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Publication details

The article was received on 09 Mar 2010, accepted on 19 May 2010 and first published on 09 Jun 2010


Article type: Paper
DOI: 10.1039/C004062B
Citation: Org. Biomol. Chem., 2010,8, 3534-3542
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    Inhibition of chorismate-utilising enzymes by 2-amino-4-carboxypyridine and 4-carboxypyridone and 5-carboxypyridone analogues

    R. J. Payne, E. M. M. Bulloch, O. Kerbarh and C. Abell, Org. Biomol. Chem., 2010, 8, 3534
    DOI: 10.1039/C004062B

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