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Your search keyword '"Clofibrate chemical synthesis"' showing total 2 results
Start Over Descriptor "Clofibrate chemical synthesis" Journal bioorganic medicinal chemistry letters
2 results on '"Clofibrate chemical synthesis"'

1. Synthesis and structure-activity relationships of fibrate-based analogues inside PPARs.

Author

Giampietro L, D'Angelo A, Giancristofaro A, Ammazzalorso A, De Filippis B, Fantacuzzi M, Linciano P, Maccallini C, and Amoroso R

Subjects
Clofibrate chemical synthesis, Clofibrate chemistry, Dose-Response Relationship, Drug, HEK293 Cells, Humans, Molecular Structure, Structure-Activity Relationship, Clofibrate pharmacology, PPAR alpha agonists, PPAR gamma agonists
Abstract

In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, new compounds based on a combination of clofibric acid, the active metabolite of clofibrate, and lipophilic groups derived from natural products chalcone and stilbene were synthesised. Some of them were found to be active at micromolar concentrations only on PPARα or PPARγ, while others were identified as dual agonists PPARα/γ., (Copyright © 2012 Elsevier Ltd. All rights reserved.)

Published
2012
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2. Synthesis of highly water-soluble fibrate derivatives via BGLation.

Author

Nemoto H, Kamiya M, Nakamoto A, Matsushita T, Matsumura K, Hattori H, Kawamura T, Taoka C, Abe S, Ishizawa K, Miyamoto L, and Tsuchiya K

Subjects
Animals, Bezafibrate blood, Bezafibrate chemical synthesis, Bezafibrate pharmacology, Clofibrate blood, Clofibrate chemical synthesis, Clofibrate pharmacology, Fenofibrate blood, Fenofibrate chemical synthesis, Fenofibrate pharmacology, Hypolipidemic Agents blood, Hypolipidemic Agents chemical synthesis, Hypolipidemic Agents pharmacology, Male, Rats, Rats, Sprague-Dawley, Solubility, Triglycerides blood, Water chemistry, Bezafibrate chemistry, Clofibrate chemistry, Fenofibrate chemistry, Hypolipidemic Agents chemistry
Abstract

Three water-soluble fibrates (fenofibrate, bezafibrate and chlofibrate) conjugated with a symmetrically branched glyceryl trimer (BGL003) were synthesized, and an evaluation of the fenofibrate-BGL003 conjugate as a candidate for anti-hyperlipemia drug was carried out using rats. The water-solubility of the fenofibrate-BGL003 conjugate was several thousand times greater than that of the original fenofibrate. The lipid-lowering effects of the fenofibrate-BGL003 conjugate were as strong as those of the same grams of fenofibrate. The actual active species of fenofibrate, fenofibric acid, was detected in rats' blood, but neither the fenofibrate-BGL003 conjugate nor fenofibrate was detected, probably due to enzymatic hydrolysis of the ester bond. The plasma concentration of fenofibric acid derived from the fenofibrate-BGL003 conjugate was five times higher than that derived from fenofibrate 4h after administration., (Copyright © 2012 Elsevier Ltd. All rights reserved.)

Published
2012
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