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2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors

Yan, Lin ; Budhu, Richard ; Huo, Pei ; Lynch, Christopher L ; Hale, Jeffrey J ; Mills, Sander G ; Hajdu, Richard ; Keohane, Carol A ; Rosenbach, Mark J ; Milligan, James A ; Shei, Gan-Ju ; Chrebet, Gary ; Bergstrom, James ; Card, Deborah ; Mandala, Suzanne M

Bioorganic & Medicinal Chemistry Letters, 01 July 2006, Vol.16(13), pp.3564-3568 [Peer Reviewed Journal]

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Title:
2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors
Author: Yan, Lin ; Budhu, Richard ; Huo, Pei ; Lynch, Christopher L ; Hale, Jeffrey J ; Mills, Sander G ; Hajdu, Richard ; Keohane, Carol A ; Rosenbach, Mark J ; Milligan, James A ; Shei, Gan-Ju ; Chrebet, Gary ; Bergstrom, James ; Card, Deborah ; Mandala, Suzanne M
Description: A series of 2-aryl(pyrrolidine-4-yl)acetic acids (e.g., ) were synthesized and evaluated as S1P receptor agonists and were found to lower peripheral lymphocyte counts in mice and to have good overall pharmacokinetic properties in rat. A series of 2-aryl(pyrrolidin-4-yl)acetic acids were synthesized and their biological activities were evaluated as agonists of S1P receptors. These analogs were able to induce lowering of lymphocyte counts in the peripheral blood of mice and were found to have good overall pharmacokinetic properties in rat.
Is Part Of: Bioorganic & Medicinal Chemistry Letters, 01 July 2006, Vol.16(13), pp.3564-3568
Identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/j.bmcl.2006.03.090
Subjects: Immunosuppressants ; S1p Agonists ; (Pyrrolidin-4-Yl)Acetic Acids ; Peripheral Lymphocyte Lowering ; Medicine ; Chemistry ; Anatomy & Physiology
Language: English

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