Article ID Journal Published Year Pages File Type
1377202 Bioorganic & Medicinal Chemistry Letters 2006 4 Pages PDF
Abstract

Based on the scaffold of (S,R)-3-(4-hydroxyphenyl)-4,5-dihydro-5-isoxazole acetic acid methyl ester (ISO-1), an inhibitor of the proinflammatory cytokine MIF, two critical modifications and chiral resolution have significantly improved the potency of the inhibition. Compound (R)-17 is 20-fold more potent than ISO-1 and inhibits MIF tautomerase activity with an IC50 of 550 nM.

Graphical abstractBased on the scaffold of ISO-1, two critical modifications and chiral resolution have significantly improved the potency of the inhibitor up to 20-folds as compared to the parent compound. Compound (R)-17 inhibits MIF tautomerase with an IC50 of 550 nM.Figure optionsDownload full-size imageDownload as PowerPoint slide

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Physical Sciences and Engineering Chemistry Organic Chemistry
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