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)=8.6muM) was discovered that suggests that this class of compounds should be evaluated further.
beta-Lactam congeners of orlistat as inhibitors of fatty acid synthase. Publishing Authors By Initials