Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377202 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
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
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kai Fan Cheng, Yousef Al-Abed,