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Bioorg Med Chem Lett. 2008 Apr 1;18(7):2491-4. doi: 10.1016/j.bmcl.2008.02.043. Epub 2008 Feb 19.

Beta-lactam congeners of orlistat as inhibitors of fatty acid synthase.

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  • 1Department of Chemistry, Texas A&M University, College Station, TX 77842-3012, USA.


Beta-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 beta-lactones, a reasonably potent, lead compound (-)-9 (IC(50)=8.6microM) was discovered that suggests that this class of compounds should be evaluated further.

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