Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1365216 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
Abstract
β-Lactam derivatives of orlistat were prepared and their inhibitory activities toward the thioesterase domain of fatty acid synthase (FAS-TE) were evaluated using a recombinant form of the enzyme. While in general these derivatives showed lower potency compared to β-lactones, a reasonably potent, lead compound (−)-9 (IC50 = 8.6 μM) was discovered that suggests that this class of compounds should be evaluated further.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Wei Zhang, Robyn D. Richardson, Supakarn Chamni, Jeffrey W. Smith, Daniel Romo,