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A series of 4-alkylamino-2-ethoxycyclobut-3en-1,2-diones has been synthesized, characterized and their inhibitory effect on pancreatic lipase (PL) was evaluated. The compound 1 has shown relatively high potency (IC50 = 0.11 mM) compared with the most effective anti-obesity drug, tetrahydrolipstatin (Orlistat) (IC50 value = 0.08 mM). The compounds have showed good selectivity toward PL and did not affect the activity of trypsin, another digestive enzyme.
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