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Synthesis and biological evaluation of orally active hypolipidemic agents. | LitMetric

Synthesis and biological evaluation of orally active hypolipidemic agents.

J Med Chem

Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur-413 255, India.

Published: August 2011

AI Article Synopsis

  • - A new series of fenofibric acid ester prodrugs (1c-1h) were created and tested to find effective treatments for lowering lipid levels in blood.
  • - Prodrugs 1c and 1d showed significant cholesterol-lowering effects, reducing plasma triglyceride levels in mice by up to 47% after an 8-day oral treatment.
  • - The prodrugs were found to be lipophilic, similar to fenofibrate, suggesting they could work well in the body for managing lipid levels.

Article Abstract

A series of novel fenofibric acid ester prodrugs 1c-1h were synthesized and evaluated with the aim of obtaining potent hypolipidemic agents. Prodrugs 1c and 1d exhibited potent hypochlolesterolemic activity, lowering the mice plasma triglyceride level up to 47% in Swiss albino mice after oral administration of 50 mg/kg/day for 8 days. Fenofibric acid ester prodrugs 1c-1h were found lipophilic like fenofibrate (1b), indicated by partition coefficients measured in octanol-buffer system at pH 7.4. On the basis of in vivo studies, prodrugs 1c and 1d emerged as potent hypolipidemic agents.

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Source
http://dx.doi.org/10.1021/jm200704fDOI Listing

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