Abstract
Pancreatic triacylglycerol lipase (PL) has been reported as an interesting pharmacological target for the management of dyslipidemia, atherosclerosis, and obesity. In the current study, a 4-quinoline-3-carboxylic acid system has been identified as a potent inhibitor of PL. Three new fluoroquinolones (11, 12, and 13) were synthesized and evaluated in vitro with respect to their anti-lipase efficacy and potency properties and gave IC50 values in the range of 18.4–29.1 μM against PL. The IC50 of the standard drug orlistat was 0.2 μM. The inhibitory activities of these compounds were supported by docking studies, which suggested that they acted according to a similar mechanism to that of the known drug orlistat. In conclusion, these effective PL inhibitors could be used to advance the development of anti-obesity drugs via the regulation of the entire gastrointestinal lipolysis process.
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