Abstract
Structure-activity relationship of sphingosine-1-phosphate receptor agonist was examined. In terms of reducing the flexibility of molecule, hit compound 1 was modified to improve S1P(1) agonistic activity as well as selectivity over S1P(3) agonistic activity. Novel S1P agonists with cinnamyl scaffold or 1,2,5,6-tetrahydropyridine scaffold were identified.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Cinnamates / chemical synthesis*
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Cinnamates / chemistry
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Fingolimod Hydrochloride
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Propylene Glycols / chemistry
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Propylene Glycols / pharmacology
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Rats
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Receptors, Lysosphingolipid / agonists*
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Sphingosine / analogs & derivatives
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Sphingosine / chemistry
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Sphingosine / pharmacology
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Structure-Activity Relationship
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beta-Alanine / chemical synthesis*
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beta-Alanine / chemistry
Substances
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Cinnamates
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Propylene Glycols
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Receptors, Lysosphingolipid
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beta-Alanine
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Fingolimod Hydrochloride
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Sphingosine