The synthesis of three isotopomers of 2-methyl-2-(4-[3-[1-(4-methylbenzyl)-5-oxo-4,5-dihydro-1H-[1,2,4]triazol-3-yl]propyl]phenoxy)propionic acid, a potent and selective peroxisome proliferator-activated receptor alpha agonist
| Autor: | Dean K. Clodfelter, Nagy A. Farid, Fengjiun Kuo, Lennon H. McKendry, William J. Wheeler |
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| Rok vydání: | 2007 |
| Předmět: |
chemistry.chemical_classification
Agonist medicine.drug_class Stereochemistry Carboxylic acid Organic Chemistry Biochemistry Chemical synthesis Analytical Chemistry Isotopomers chemistry Nuclear receptor Drug Discovery medicine Radiology Nuclear Medicine and imaging Peroxisome proliferator-activated receptor alpha Receptor Spectroscopy ADME |
| Zdroj: | Journal of Labelled Compounds and Radiopharmaceuticals. 50:693-701 |
| ISSN: | 1099-1344 0362-4803 |
| Popis: | Although fenofibrate (1a) is commercially available and clinically effective in lowering serum triglycerides, its activity and sub-type selectivity at the PPARα receptors are only moderate; therefore, there exists a need for more potent and sub-type selective PPARα agonists. To that end, discovery efforts have identified 2-methyl-2-(4-[3-[1-(4-methylbenzyl)-5-oxo-4,5-dihydro-1H-[1,2,4]triazol-3-yl]propyl]phenoxy)propionic acid (2), a potent and selective human PPARα receptor agonist. In support of pre-clinical ADME studies and bioanalysis, three isotopomers of 2 have been synthesized. The results of these efforts are described below. Copyright © 2007 John Wiley & Sons, Ltd. |
| Databáze: | OpenAIRE |
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