2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors
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. A series of 2-aryl(pyrrolidin-4-yl)acetic acids were synthesiz...
Gespeichert in:
| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2006-07, Vol.16 (13), p.3564-3568 |
|---|---|
| Hauptverfasser: | , , , , , , , , , , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 3568 |
|---|---|
| container_issue | 13 |
| container_start_page | 3564 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 16 |
| creator | 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., 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.
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. |
| doi_str_mv | 10.1016/j.bmcl.2006.03.090 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_68027802</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0960894X06003878</els_id><sourcerecordid>68027802</sourcerecordid><originalsourceid>FETCH-LOGICAL-c415t-4e9fdd14880f27721576d6d8d7565284f959e01aa530574125c4feb112887a3d3</originalsourceid><addsrcrecordid>eNqFkU-LFDEQxYMo7uzqF_AgfVF2D2kr6fxr2MuyuCosKKjgLWSS6t0MPZ026RHm25thBvamh6Kg-L3i8R4hbxi0DJj6sGnXWz-2HEC10LXQwzOyYkIJ2gmQz8kKegXU9OLXGTkvZQPABAjxkpwxpTiToluRNac3eT9ezvuc0xhDnKig-_HKeVyib5yPoTQuYzOnBaelcQ9pimUpTRqaMj_G6SGVOCFldH5M9eAWbC6_s29XTUaP85JyeUVeDG4s-Pq0L8jPu48_bj_T-6-fvtze3FMvmFyowH4IgQljYOBaV39aBRVM0FJJbsTQyx6BOSc7kFowLr0YcM0YN0a7LnQX5P3x75zT7x2WxW5j8TiObsK0K1YZ4LrOf0GmmVZGmgryI-hzKiXjYOccty7vLQN7qMBu7KECe6jAQmdrBVX09vR9t95ieJKcMq_AuxPginfjkN3kY3niqkfgQlfu-shhDe1PxGyLjzh5DLFmu9iQ4r98_AUYpKLN</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>17176858</pqid></control><display><type>article</type><title>2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors</title><source>MEDLINE</source><source>Access via ScienceDirect (Elsevier)</source><creator>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.</creator><creatorcontrib>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.</creatorcontrib><description>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.
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.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2006.03.090</identifier><identifier>PMID: 16621543</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>(Pyrrolidin-4-yl)acetic acids ; Acetates - chemical synthesis ; Acetates - chemistry ; Acetates - pharmacology ; Animals ; Biological and medical sciences ; Immunomodulators ; Immunosuppressants ; Lymphocyte Count ; Lysophospholipids - antagonists & inhibitors ; Medical sciences ; Mice ; Molecular Structure ; Peripheral lymphocyte lowering ; Pharmacology. Drug treatments ; Protein Binding - drug effects ; Pyrrolidines - chemical synthesis ; Pyrrolidines - chemistry ; Pyrrolidines - pharmacology ; Rats ; Receptors, Lysosphingolipid - agonists ; S1P agonists ; Sphingosine - analogs & derivatives ; Sphingosine - antagonists & inhibitors ; Stereoisomerism ; Structure-Activity Relationship</subject><ispartof>Bioorganic & medicinal chemistry letters, 2006-07, Vol.16 (13), p.3564-3568</ispartof><rights>2006 Elsevier Ltd</rights><rights>2006 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c415t-4e9fdd14880f27721576d6d8d7565284f959e01aa530574125c4feb112887a3d3</citedby><cites>FETCH-LOGICAL-c415t-4e9fdd14880f27721576d6d8d7565284f959e01aa530574125c4feb112887a3d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2006.03.090$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=17800247$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/16621543$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Yan, Lin</creatorcontrib><creatorcontrib>Budhu, Richard</creatorcontrib><creatorcontrib>Huo, Pei</creatorcontrib><creatorcontrib>Lynch, Christopher L.</creatorcontrib><creatorcontrib>Hale, Jeffrey J.</creatorcontrib><creatorcontrib>Mills, Sander G.</creatorcontrib><creatorcontrib>Hajdu, Richard</creatorcontrib><creatorcontrib>Keohane, Carol A.</creatorcontrib><creatorcontrib>Rosenbach, Mark J.</creatorcontrib><creatorcontrib>Milligan, James A.</creatorcontrib><creatorcontrib>Shei, Gan-Ju</creatorcontrib><creatorcontrib>Chrebet, Gary</creatorcontrib><creatorcontrib>Bergstrom, James</creatorcontrib><creatorcontrib>Card, Deborah</creatorcontrib><creatorcontrib>Mandala, Suzanne M.</creatorcontrib><title>2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>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.
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.</description><subject>(Pyrrolidin-4-yl)acetic acids</subject><subject>Acetates - chemical synthesis</subject><subject>Acetates - chemistry</subject><subject>Acetates - pharmacology</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Immunomodulators</subject><subject>Immunosuppressants</subject><subject>Lymphocyte Count</subject><subject>Lysophospholipids - antagonists & inhibitors</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Molecular Structure</subject><subject>Peripheral lymphocyte lowering</subject><subject>Pharmacology. Drug treatments</subject><subject>Protein Binding - drug effects</subject><subject>Pyrrolidines - chemical synthesis</subject><subject>Pyrrolidines - chemistry</subject><subject>Pyrrolidines - pharmacology</subject><subject>Rats</subject><subject>Receptors, Lysosphingolipid - agonists</subject><subject>S1P agonists</subject><subject>Sphingosine - analogs & derivatives</subject><subject>Sphingosine - antagonists & inhibitors</subject><subject>Stereoisomerism</subject><subject>Structure-Activity Relationship</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2006</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU-LFDEQxYMo7uzqF_AgfVF2D2kr6fxr2MuyuCosKKjgLWSS6t0MPZ026RHm25thBvamh6Kg-L3i8R4hbxi0DJj6sGnXWz-2HEC10LXQwzOyYkIJ2gmQz8kKegXU9OLXGTkvZQPABAjxkpwxpTiToluRNac3eT9ezvuc0xhDnKig-_HKeVyib5yPoTQuYzOnBaelcQ9pimUpTRqaMj_G6SGVOCFldH5M9eAWbC6_s29XTUaP85JyeUVeDG4s-Pq0L8jPu48_bj_T-6-fvtze3FMvmFyowH4IgQljYOBaV39aBRVM0FJJbsTQyx6BOSc7kFowLr0YcM0YN0a7LnQX5P3x75zT7x2WxW5j8TiObsK0K1YZ4LrOf0GmmVZGmgryI-hzKiXjYOccty7vLQN7qMBu7KECe6jAQmdrBVX09vR9t95ieJKcMq_AuxPginfjkN3kY3niqkfgQlfu-shhDe1PxGyLjzh5DLFmu9iQ4r98_AUYpKLN</recordid><startdate>20060701</startdate><enddate>20060701</enddate><creator>Yan, Lin</creator><creator>Budhu, Richard</creator><creator>Huo, Pei</creator><creator>Lynch, Christopher L.</creator><creator>Hale, Jeffrey J.</creator><creator>Mills, Sander G.</creator><creator>Hajdu, Richard</creator><creator>Keohane, Carol A.</creator><creator>Rosenbach, Mark J.</creator><creator>Milligan, James A.</creator><creator>Shei, Gan-Ju</creator><creator>Chrebet, Gary</creator><creator>Bergstrom, James</creator><creator>Card, Deborah</creator><creator>Mandala, Suzanne M.</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20060701</creationdate><title>2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors</title><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.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c415t-4e9fdd14880f27721576d6d8d7565284f959e01aa530574125c4feb112887a3d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2006</creationdate><topic>(Pyrrolidin-4-yl)acetic acids</topic><topic>Acetates - chemical synthesis</topic><topic>Acetates - chemistry</topic><topic>Acetates - pharmacology</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Immunomodulators</topic><topic>Immunosuppressants</topic><topic>Lymphocyte Count</topic><topic>Lysophospholipids - antagonists & inhibitors</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Molecular Structure</topic><topic>Peripheral lymphocyte lowering</topic><topic>Pharmacology. Drug treatments</topic><topic>Protein Binding - drug effects</topic><topic>Pyrrolidines - chemical synthesis</topic><topic>Pyrrolidines - chemistry</topic><topic>Pyrrolidines - pharmacology</topic><topic>Rats</topic><topic>Receptors, Lysosphingolipid - agonists</topic><topic>S1P agonists</topic><topic>Sphingosine - analogs & derivatives</topic><topic>Sphingosine - antagonists & inhibitors</topic><topic>Stereoisomerism</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Yan, Lin</creatorcontrib><creatorcontrib>Budhu, Richard</creatorcontrib><creatorcontrib>Huo, Pei</creatorcontrib><creatorcontrib>Lynch, Christopher L.</creatorcontrib><creatorcontrib>Hale, Jeffrey J.</creatorcontrib><creatorcontrib>Mills, Sander G.</creatorcontrib><creatorcontrib>Hajdu, Richard</creatorcontrib><creatorcontrib>Keohane, Carol A.</creatorcontrib><creatorcontrib>Rosenbach, Mark J.</creatorcontrib><creatorcontrib>Milligan, James A.</creatorcontrib><creatorcontrib>Shei, Gan-Ju</creatorcontrib><creatorcontrib>Chrebet, Gary</creatorcontrib><creatorcontrib>Bergstrom, James</creatorcontrib><creatorcontrib>Card, Deborah</creatorcontrib><creatorcontrib>Mandala, Suzanne M.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Yan, Lin</au><au>Budhu, Richard</au><au>Huo, Pei</au><au>Lynch, Christopher L.</au><au>Hale, Jeffrey J.</au><au>Mills, Sander G.</au><au>Hajdu, Richard</au><au>Keohane, Carol A.</au><au>Rosenbach, Mark J.</au><au>Milligan, James A.</au><au>Shei, Gan-Ju</au><au>Chrebet, Gary</au><au>Bergstrom, James</au><au>Card, Deborah</au><au>Mandala, Suzanne M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2006-07-01</date><risdate>2006</risdate><volume>16</volume><issue>13</issue><spage>3564</spage><epage>3568</epage><pages>3564-3568</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><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.
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.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>16621543</pmid><doi>10.1016/j.bmcl.2006.03.090</doi><tpages>5</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2006-07, Vol.16 (13), p.3564-3568 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_68027802 |
| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | (Pyrrolidin-4-yl)acetic acids Acetates - chemical synthesis Acetates - chemistry Acetates - pharmacology Animals Biological and medical sciences Immunomodulators Immunosuppressants Lymphocyte Count Lysophospholipids - antagonists & inhibitors Medical sciences Mice Molecular Structure Peripheral lymphocyte lowering Pharmacology. Drug treatments Protein Binding - drug effects Pyrrolidines - chemical synthesis Pyrrolidines - chemistry Pyrrolidines - pharmacology Rats Receptors, Lysosphingolipid - agonists S1P agonists Sphingosine - analogs & derivatives Sphingosine - antagonists & inhibitors Stereoisomerism Structure-Activity Relationship |
| title | 2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-25T17%3A38%3A54IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=2-Aryl(pyrrolidin-4-yl)acetic%20acids%20are%20potent%20agonists%20of%20sphingosine-1-phosphate%20(S1P)%20receptors&rft.jtitle=Bioorganic%20&%20medicinal%20chemistry%20letters&rft.au=Yan,%20Lin&rft.date=2006-07-01&rft.volume=16&rft.issue=13&rft.spage=3564&rft.epage=3568&rft.pages=3564-3568&rft.issn=0960-894X&rft.eissn=1464-3405&rft_id=info:doi/10.1016/j.bmcl.2006.03.090&rft_dat=%3Cproquest_cross%3E68027802%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=17176858&rft_id=info:pmid/16621543&rft_els_id=S0960894X06003878&rfr_iscdi=true |