Synthesis of a novel human PPARδ selective agonist and its stimulatory effect on oligodendrocyte differentiation
We have succeeded in synthesizing a novel PPARδ selective agonist, compound 20, characterized by a benzisoxazole ring. Compound 20 exhibited a potent hPPARδ transactivation activity and high δ selectivity. Compound 20 stimulated oligodendrocyte differentiation of primary oligodendrocyte precursors c...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2011-01, Vol.21 (1), p.240-244 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Sakuma, Shogo Endo, Tsuyoshi Kanda, Takashi Nakamura, Hideki Yamasaki, Satomi Yamakawa, Tomio |
| description | We have succeeded in synthesizing a novel PPARδ selective agonist, compound 20, characterized by a benzisoxazole ring. Compound 20 exhibited a potent hPPARδ transactivation activity and high δ selectivity. Compound 20 stimulated oligodendrocyte differentiation of primary oligodendrocyte precursors cells in vitro, indicating that it may be an effective drug to treat demyelinating disorders, such as multiple sclerosis.
We successfully synthesized a novel peroxisome proliferator-activated receptor (PPAR)δ selective agonist, namely, compound 20, with a characteristic benzisoxazole ring. Compound 20 exhibited potent human PPARδ transactivation activity and high δ selectivity. Further, it stimulated differentiation of primary oligodendrocyte precursor cells in vitro, indicating that it may be an effective drug in the treatment of demyelinating disorders such as multiple sclerosis. |
| doi_str_mv | 10.1016/j.bmcl.2010.11.030 |
| format | Article |
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We successfully synthesized a novel peroxisome proliferator-activated receptor (PPAR)δ selective agonist, namely, compound 20, with a characteristic benzisoxazole ring. Compound 20 exhibited potent human PPARδ transactivation activity and high δ selectivity. Further, it stimulated differentiation of primary oligodendrocyte precursor cells in vitro, indicating that it may be an effective drug in the treatment of demyelinating disorders such as multiple sclerosis.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2010.11.030</identifier><identifier>PMID: 21112784</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>agonists ; Animals ; Benzisoxazole ring ; Biological and medical sciences ; Brain - pathology ; Cell Differentiation ; Compound 20 ; drug therapy ; Humans ; Isoxazoles - chemical synthesis ; Isoxazoles - chemistry ; Isoxazoles - therapeutic use ; Medical sciences ; Miscellaneous ; Multiple sclerosis ; Multiple Sclerosis - drug therapy ; Neuropharmacology ; Oligodendrocyte ; Oligodendroglia - cytology ; Oxazoles - chemical synthesis ; Oxazoles - chemistry ; Oxazoles - therapeutic use ; Pharmacology. Drug treatments ; PPAR delta - agonists ; PPAR delta - metabolism ; PPARδ agonist ; Rats ; sclerosis ; Transcriptional Activation</subject><ispartof>Bioorganic & medicinal chemistry letters, 2011-01, Vol.21 (1), p.240-244</ispartof><rights>2010 Elsevier Ltd</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2010 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c441t-192addb560f52eae40b742e0fbb23d2593c670ef8e1888563d4f457843b7424a3</citedby><cites>FETCH-LOGICAL-c441t-192addb560f52eae40b742e0fbb23d2593c670ef8e1888563d4f457843b7424a3</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.2010.11.030$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,4024,27923,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=23726791$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/21112784$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Sakuma, Shogo</creatorcontrib><creatorcontrib>Endo, Tsuyoshi</creatorcontrib><creatorcontrib>Kanda, Takashi</creatorcontrib><creatorcontrib>Nakamura, Hideki</creatorcontrib><creatorcontrib>Yamasaki, Satomi</creatorcontrib><creatorcontrib>Yamakawa, Tomio</creatorcontrib><title>Synthesis of a novel human PPARδ selective agonist and its stimulatory effect on oligodendrocyte differentiation</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>We have succeeded in synthesizing a novel PPARδ selective agonist, compound 20, characterized by a benzisoxazole ring. Compound 20 exhibited a potent hPPARδ transactivation activity and high δ selectivity. Compound 20 stimulated oligodendrocyte differentiation of primary oligodendrocyte precursors cells in vitro, indicating that it may be an effective drug to treat demyelinating disorders, such as multiple sclerosis.
We successfully synthesized a novel peroxisome proliferator-activated receptor (PPAR)δ selective agonist, namely, compound 20, with a characteristic benzisoxazole ring. Compound 20 exhibited potent human PPARδ transactivation activity and high δ selectivity. Further, it stimulated differentiation of primary oligodendrocyte precursor cells in vitro, indicating that it may be an effective drug in the treatment of demyelinating disorders such as multiple sclerosis.</description><subject>agonists</subject><subject>Animals</subject><subject>Benzisoxazole ring</subject><subject>Biological and medical sciences</subject><subject>Brain - pathology</subject><subject>Cell Differentiation</subject><subject>Compound 20</subject><subject>drug therapy</subject><subject>Humans</subject><subject>Isoxazoles - chemical synthesis</subject><subject>Isoxazoles - chemistry</subject><subject>Isoxazoles - therapeutic use</subject><subject>Medical sciences</subject><subject>Miscellaneous</subject><subject>Multiple sclerosis</subject><subject>Multiple Sclerosis - drug therapy</subject><subject>Neuropharmacology</subject><subject>Oligodendrocyte</subject><subject>Oligodendroglia - cytology</subject><subject>Oxazoles - chemical synthesis</subject><subject>Oxazoles - chemistry</subject><subject>Oxazoles - therapeutic use</subject><subject>Pharmacology. Drug treatments</subject><subject>PPAR delta - agonists</subject><subject>PPAR delta - metabolism</subject><subject>PPARδ agonist</subject><subject>Rats</subject><subject>sclerosis</subject><subject>Transcriptional Activation</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkc1qVDEYhoModlq9AReaTenqjPk7f-CmFP-gYLEW3IWc5Ms0wzlJm-QMzH15HV6TOcyoO10Fkud7k7wPQq8oWVNCm7fb9TDpcc3IskHXhJMnaEVFIyouSP0UrUjfkKrrxfcTdJrSlhAqiBDP0QmjlLK2Eyv0eLv3-R6SSzhYrLAPOxjx_Twpj29uLr_-_IETjKCz2wFWm-Bdylh5g11OOGU3zaPKIe4xWFsoHDwOo9sEA97EoPcZsHHlKILPTmUX_Av0zKoxwcvjeobuPrz_dvWpuv7y8fPV5XWlhaC5oj1Txgx1Q2zNQIEgQysYEDsMjBtW91w3LQHbAe26rm64EVbU5U984YTiZ-jikPsQw-MMKcvJJQ3jqDyEOcmu46WPvib_J0tdfUdYU0h2IHUMKUWw8iG6ScW9pEQuTuRWLk7k4kRSKouTMvT6GD8PE5g_I78lFOD8CKik1Wij8tqlvxxvWdP2tHBvDpxVQapNLMzdbbmpLmK5YGxJencgoBS7cxBl0g68BuNisSNNcP966S9vzLTV</recordid><startdate>20110101</startdate><enddate>20110101</enddate><creator>Sakuma, Shogo</creator><creator>Endo, Tsuyoshi</creator><creator>Kanda, Takashi</creator><creator>Nakamura, Hideki</creator><creator>Yamasaki, Satomi</creator><creator>Yamakawa, Tomio</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>FBQ</scope><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>7X8</scope><scope>7QO</scope><scope>7TK</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20110101</creationdate><title>Synthesis of a novel human PPARδ selective agonist and its stimulatory effect on oligodendrocyte differentiation</title><author>Sakuma, Shogo ; Endo, Tsuyoshi ; Kanda, Takashi ; Nakamura, Hideki ; Yamasaki, Satomi ; Yamakawa, Tomio</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c441t-192addb560f52eae40b742e0fbb23d2593c670ef8e1888563d4f457843b7424a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2011</creationdate><topic>agonists</topic><topic>Animals</topic><topic>Benzisoxazole ring</topic><topic>Biological and medical sciences</topic><topic>Brain - pathology</topic><topic>Cell Differentiation</topic><topic>Compound 20</topic><topic>drug therapy</topic><topic>Humans</topic><topic>Isoxazoles - chemical synthesis</topic><topic>Isoxazoles - chemistry</topic><topic>Isoxazoles - therapeutic use</topic><topic>Medical sciences</topic><topic>Miscellaneous</topic><topic>Multiple sclerosis</topic><topic>Multiple Sclerosis - drug therapy</topic><topic>Neuropharmacology</topic><topic>Oligodendrocyte</topic><topic>Oligodendroglia - cytology</topic><topic>Oxazoles - chemical synthesis</topic><topic>Oxazoles - chemistry</topic><topic>Oxazoles - therapeutic use</topic><topic>Pharmacology. Drug treatments</topic><topic>PPAR delta - agonists</topic><topic>PPAR delta - metabolism</topic><topic>PPARδ agonist</topic><topic>Rats</topic><topic>sclerosis</topic><topic>Transcriptional Activation</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Sakuma, Shogo</creatorcontrib><creatorcontrib>Endo, Tsuyoshi</creatorcontrib><creatorcontrib>Kanda, Takashi</creatorcontrib><creatorcontrib>Nakamura, Hideki</creatorcontrib><creatorcontrib>Yamasaki, Satomi</creatorcontrib><creatorcontrib>Yamakawa, Tomio</creatorcontrib><collection>AGRIS</collection><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>MEDLINE - Academic</collection><collection>Biotechnology Research Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Sakuma, Shogo</au><au>Endo, Tsuyoshi</au><au>Kanda, Takashi</au><au>Nakamura, Hideki</au><au>Yamasaki, Satomi</au><au>Yamakawa, Tomio</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis of a novel human PPARδ selective agonist and its stimulatory effect on oligodendrocyte differentiation</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2011-01-01</date><risdate>2011</risdate><volume>21</volume><issue>1</issue><spage>240</spage><epage>244</epage><pages>240-244</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>We have succeeded in synthesizing a novel PPARδ selective agonist, compound 20, characterized by a benzisoxazole ring. Compound 20 exhibited a potent hPPARδ transactivation activity and high δ selectivity. Compound 20 stimulated oligodendrocyte differentiation of primary oligodendrocyte precursors cells in vitro, indicating that it may be an effective drug to treat demyelinating disorders, such as multiple sclerosis.
We successfully synthesized a novel peroxisome proliferator-activated receptor (PPAR)δ selective agonist, namely, compound 20, with a characteristic benzisoxazole ring. Compound 20 exhibited potent human PPARδ transactivation activity and high δ selectivity. Further, it stimulated differentiation of primary oligodendrocyte precursor cells in vitro, indicating that it may be an effective drug in the treatment of demyelinating disorders such as multiple sclerosis.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>21112784</pmid><doi>10.1016/j.bmcl.2010.11.030</doi><tpages>5</tpages></addata></record> |
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| subjects | agonists Animals Benzisoxazole ring Biological and medical sciences Brain - pathology Cell Differentiation Compound 20 drug therapy Humans Isoxazoles - chemical synthesis Isoxazoles - chemistry Isoxazoles - therapeutic use Medical sciences Miscellaneous Multiple sclerosis Multiple Sclerosis - drug therapy Neuropharmacology Oligodendrocyte Oligodendroglia - cytology Oxazoles - chemical synthesis Oxazoles - chemistry Oxazoles - therapeutic use Pharmacology. Drug treatments PPAR delta - agonists PPAR delta - metabolism PPARδ agonist Rats sclerosis Transcriptional Activation |
| title | Synthesis of a novel human PPARδ selective agonist and its stimulatory effect on oligodendrocyte differentiation |
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