Article ID Journal Published Year Pages File Type
1365216 Bioorganic & Medicinal Chemistry Letters 2008 4 Pages PDF
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
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