Journal of Enzyme Inhibition and Medicinal Chemistry 2011-08-01

Evaluation of the inhibitory potential of five squaric acid derivatives against pancreatic lipase.

Zorka Bobcheva, Diana Zhiryakova, Maya Guncheva

Index: J. Enzyme Inhib. Med. Chem. 26(4) , 587-91, (2011)

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Abstract

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 (IC(50) = 0.11 mM) compared with the most effective anti-obesity drug, tetrahydrolipstatin (Orlistat) (IC(50) value = 0.08 mM). The compounds have showed good selectivity toward PL and did not affect the activity of trypsin, another digestive enzyme.