title: Evaluation of the inhibitory potential of five squaric acid derivatives against pancreatic lipase.
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.
authors: Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Sofia, Bulgaria.
authors: Zorka
authors: Z
authors: Bobcheva
authors: Diana
authors: D
authors: Zhiryakova
authors: Maya
authors: M
authors: Guncheva
mesh_terms: D003503:Cyclobutanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008049:Lipase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015394:Molecular Structure; D010179:Pancreas / Q000201:enzymology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014357:Trypsin / Q000378:metabolism
chemical_list: D003503:Cyclobutanes; D004791:Enzyme Inhibitors; D008049:Lipase; D014357:Trypsin; C030042:squaric acid