Intermediate analogue inhibitors of mandelate racemase: N-Hydroxyformanilide and cupferron.
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Bourque JR, Burley RK, Bearne SL
Intermediate analogue inhibitors of mandelate racemase: N-Hydroxyformanilide and cupferron.
Bioorg Med Chem Lett. 2007 Jan 1;17(1):105-8. Epub 2006 Sep 30.
- PubMed ID
- 17055725 [ View in PubMed]
- Abstract
Mandelate racemase (MR) catalyzes the 1,1-proton transfer that interconverts the enantiomers of mandelate. The transition state/intermediate analogues N-hydroxyformanilide (K(i)=2.79+/-0.19 microM) and cupferron (K(i)=2.67+/-0.09 microM) are identified as potent competitive inhibitors of MR. The pH-pK(i) profile indicates that MR can bind either the protonated or deprotonated forms of N-hydroxyformanilide, with a 10-fold greater affinity for the latter form.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) (S)-Mandelic acid Mandelate racemase Ki (nM) 810000 N/A N/A Details