Abstract
A practical method of synthesizing a highly selective EP4-receptor agonist 1 using Corey lactone 2 as a key intermediate was developed. Selective methanesulfonylation of the primary alcohol of the diol 8 under the newly devised conditions followed by the protection of the remaining secondary alcohol are key reactions in this new method. Further biological evaluation of 1a-b is also reported.
MeSH terms
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Animals
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Blood Cells / drug effects
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Blood Cells / metabolism
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Humans
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Interleukin-10 / biosynthesis
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Interleukin-10 / blood
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Lipopolysaccharides / pharmacology
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Rats
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Receptors, Prostaglandin E / agonists*
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Receptors, Prostaglandin E, EP4 Subtype
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Signal Transduction
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Spectrum Analysis
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Tumor Necrosis Factor-alpha / metabolism
Substances
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Lipopolysaccharides
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PTGER4 protein, human
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Receptors, Prostaglandin E
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Receptors, Prostaglandin E, EP4 Subtype
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Tumor Necrosis Factor-alpha
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Interleukin-10