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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, 07/2006, 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: To link to full-text access for this article, visit this link: http://dx.doi.org/10.1016/j.bmcl.2006.03.090 Byline: Lin Yan (a), Richard Budhu (a), Pei Huo (a), Christopher L. Lynch (a), Jeffrey J. Hale (a), Sander G. Mills (a), Richard Hajdu (b), Carol A. Keohane (b), Mark J. Rosenbach (b), James A. Milligan (b), Gan-Ju Shei (b), Gary Chrebet (b), James Bergstrom (b), Deborah Card (b), Suzanne M. Mandala (b) Keywords: Immunosuppressants; S1P agonists; (Pyrrolidin-4-yl)acetic acids; Peripheral lymphocyte lowering Abstract: A series of 2-aryl(pyrrolidine-4-yl)acetic acids (e.g., 22g) 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. Author Affiliation: (a) Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA (b) Department of Immunology and Rheumatology, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA Article History: Received 18 January 2006; Revised 23 March 2006; Accepted 24 March 2006
  • Is Part Of: Bioorganic & Medicinal Chemistry Letters, 07/2006, Vol.16(13), pp.3564-3568
  • Identifier: ISSN: 0960894X ; DOI: http://dx.doi.org/10.1016/j.bmcl.2006.03.090
  • Subjects: Immunosuppressive Agents ; Phosphates ; Lymphocytes ; Sphingosine ; Acetic Acid
  • Language: English

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