Synthesis of an Urea-substituted Selenoisobutyric Acid Isostere of the Peroxisome Proliferator-activated Receptor α Selective Agonist

Title
Synthesis of an Urea-substituted Selenoisobutyric Acid Isostere of the Peroxisome Proliferator-activated Receptor α Selective Agonist
Authors
황후상최혁재남상집고재영함정엽진정욱강헌중
Keywords
PPARα; GW7647; Bioisosterism; Alkyl selenide
Issue Date
2011-11
Publisher
Bulletin of the Korean Chemical Society
Citation
VOL 32, NO 11, 4089-4091
Abstract
Peroxisome Proliferator-Activated Receptor α (PPARα), a major regulator of energy homeostasis discovered in 1990, is present at high density in the liver and regulates the expression of genes involved in fatty acid β-oxidation.1 As research on its function has been localized to animal experiments, the function of PPARα in humans is still unclear. Past studies revealed PPARα participation in tumorgenesis,2 inflammation3,4 and atherosclerosis.5 Therefore, selective agonists of PPARα are expected to be potential antitumor, anti-inflammatory and anti-atherosclerotic agents. Fibrates were the first generation of PPARα modulators (Figure 1) GlaxoSmithKline (GSK) then developed a series of ureasubstituted thioisobutyric acids (ureido-TiBAs),6 which were synthesized using a parallel-array synthetic method. Ureido- TiBA derivatives synthesized from the compounds GW7647 and GW9578 were found to be effective for heart disease caused by hypertension and high-cholesterol in vivo (Figure 2).
URI
http://pubs.kist.re.kr/handle/201004/40728
ISSN
0253-2964
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KIST Publication > Article
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