Abstract
Various carboxylic acids, phosphonic acids, sulfonic acids, tetrazoles as well as sulfonylhydantoins were prepared as phosphate mimics of the chiral aminophosphate 1-P to act as agonists on the S1P(1) receptor. It was found that amino phosphonates and amino carboxylates are potent S1P(1) binders. beta-Amino acid 11 could be shown to reversibly reduce blood lymphocyte counts in rats after po administration.
Copyright 2010 Elsevier Ltd. All rights reserved.
MeSH terms
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Administration, Oral
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Amino Acids / chemistry
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Animals
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Fingolimod Hydrochloride
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Immunosuppressive Agents / chemical synthesis
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Immunosuppressive Agents / chemistry*
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Immunosuppressive Agents / pharmacology
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Isoleucine / analogs & derivatives*
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Isoleucine / chemical synthesis
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Isoleucine / chemistry
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Isoleucine / pharmacology
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Lymphocytes / drug effects
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Lymphocytes / immunology
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Phosphates / chemistry*
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Phosphorylation
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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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Receptors, Lysosphingolipid / metabolism
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Sphingosine / analogs & derivatives*
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Sphingosine / chemistry
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Sphingosine / pharmacology
Substances
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Amino Acids
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Immunosuppressive Agents
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Phosphates
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Propylene Glycols
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Receptors, Lysosphingolipid
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Isoleucine
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Fingolimod Hydrochloride
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Sphingosine