The discovery of a potent Nav1.3 inhibitor with good oral pharmacokineticsAll authors are, or were at the time of the work being undertaken, employees of Pfizer
In this article, we describe the discovery of an aryl ether series of potent and selective Na v 1.3 inhibitors. Based on structural analogy to a similar series of compounds we have previously shown bind to the domain IV voltage sensor region of Na v channels, we propose this series binds in the same...
Gespeichert in:
| Hauptverfasser: | , , , , , , , , , , , , , , |
|---|---|
| Format: | Artikel |
| Sprache: | eng |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 1267 |
|---|---|
| container_issue | 6 |
| container_start_page | 1255 |
| container_title | |
| container_volume | 8 |
| creator | Pryde, D. C Swain, N. A Stupple, P. A West, C. W Marron, B Markworth, C. J Printzenhoff, D Lin, Z Cox, P. J Suzuki, R McMurray, S Waldron, G. J Payne, C. E Warmus, J. S Chapman, M. L |
| description | In this article, we describe the discovery of an aryl ether series of potent and selective Na
v
1.3 inhibitors. Based on structural analogy to a similar series of compounds we have previously shown bind to the domain IV voltage sensor region of Na
v
channels, we propose this series binds in the same location. We describe the development of this series from a published starting point, highlighting key selectivity and potency data, and several studies designed to validate Na
v
1.3 as a target for pain.
An aryl ether series of potent and selective Na
v
1.3 inhibitors is described, starting from a series of diphenymethyl amides. |
| doi_str_mv | 10.1039/c7md00131b |
| format | Article |
| fullrecord | <record><control><sourceid>rsc</sourceid><recordid>TN_cdi_rsc_primary_c7md00131b</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>c7md00131b</sourcerecordid><originalsourceid>FETCH-rsc_primary_c7md00131b3</originalsourceid><addsrcrecordid>eNqFT8FKw0AUXETBor14F573tu5mK7ZHEcWTeOg9vCQv3TXJvvB22xK_xk-1AdGbzmUGZoZhlLoyemG0Xd-W912ltbGmOFGTTC_1PLsz5vRHa3uupjG-6yNstlqtlxP1uXEElY8l70kG4BoQek4UErzi3iws-OB84RMLHHxysGWugAVb6B1KhyU3PlDyZXxoW8BdciwRUGgGY4WEABOk40ryHY0Doz6wNFCQD1vYhYokYUNhBtT1LQ9Eccy91f6D5FKd1dhGmn7zhbp-fto8vswllnkvvkMZ8t_n9n__5i8_76vafgHJ8Wlg</addsrcrecordid><sourcetype>Enrichment Source</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype></control><display><type>article</type><title>The discovery of a potent Nav1.3 inhibitor with good oral pharmacokineticsAll authors are, or were at the time of the work being undertaken, employees of Pfizer</title><source>Royal Society Of Chemistry Journals 2008-</source><source>PubMed Central</source><creator>Pryde, D. C ; Swain, N. A ; Stupple, P. A ; West, C. W ; Marron, B ; Markworth, C. J ; Printzenhoff, D ; Lin, Z ; Cox, P. J ; Suzuki, R ; McMurray, S ; Waldron, G. J ; Payne, C. E ; Warmus, J. S ; Chapman, M. L</creator><creatorcontrib>Pryde, D. C ; Swain, N. A ; Stupple, P. A ; West, C. W ; Marron, B ; Markworth, C. J ; Printzenhoff, D ; Lin, Z ; Cox, P. J ; Suzuki, R ; McMurray, S ; Waldron, G. J ; Payne, C. E ; Warmus, J. S ; Chapman, M. L</creatorcontrib><description>In this article, we describe the discovery of an aryl ether series of potent and selective Na
v
1.3 inhibitors. Based on structural analogy to a similar series of compounds we have previously shown bind to the domain IV voltage sensor region of Na
v
channels, we propose this series binds in the same location. We describe the development of this series from a published starting point, highlighting key selectivity and potency data, and several studies designed to validate Na
v
1.3 as a target for pain.
An aryl ether series of potent and selective Na
v
1.3 inhibitors is described, starting from a series of diphenymethyl amides.</description><identifier>ISSN: 2040-2503</identifier><identifier>EISSN: 2040-2511</identifier><identifier>DOI: 10.1039/c7md00131b</identifier><language>eng</language><creationdate>2017-06</creationdate><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids></links><search><creatorcontrib>Pryde, D. C</creatorcontrib><creatorcontrib>Swain, N. A</creatorcontrib><creatorcontrib>Stupple, P. A</creatorcontrib><creatorcontrib>West, C. W</creatorcontrib><creatorcontrib>Marron, B</creatorcontrib><creatorcontrib>Markworth, C. J</creatorcontrib><creatorcontrib>Printzenhoff, D</creatorcontrib><creatorcontrib>Lin, Z</creatorcontrib><creatorcontrib>Cox, P. J</creatorcontrib><creatorcontrib>Suzuki, R</creatorcontrib><creatorcontrib>McMurray, S</creatorcontrib><creatorcontrib>Waldron, G. J</creatorcontrib><creatorcontrib>Payne, C. E</creatorcontrib><creatorcontrib>Warmus, J. S</creatorcontrib><creatorcontrib>Chapman, M. L</creatorcontrib><title>The discovery of a potent Nav1.3 inhibitor with good oral pharmacokineticsAll authors are, or were at the time of the work being undertaken, employees of Pfizer</title><description>In this article, we describe the discovery of an aryl ether series of potent and selective Na
v
1.3 inhibitors. Based on structural analogy to a similar series of compounds we have previously shown bind to the domain IV voltage sensor region of Na
v
channels, we propose this series binds in the same location. We describe the development of this series from a published starting point, highlighting key selectivity and potency data, and several studies designed to validate Na
v
1.3 as a target for pain.
An aryl ether series of potent and selective Na
v
1.3 inhibitors is described, starting from a series of diphenymethyl amides.</description><issn>2040-2503</issn><issn>2040-2511</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid/><recordid>eNqFT8FKw0AUXETBor14F573tu5mK7ZHEcWTeOg9vCQv3TXJvvB22xK_xk-1AdGbzmUGZoZhlLoyemG0Xd-W912ltbGmOFGTTC_1PLsz5vRHa3uupjG-6yNstlqtlxP1uXEElY8l70kG4BoQek4UErzi3iws-OB84RMLHHxysGWugAVb6B1KhyU3PlDyZXxoW8BdciwRUGgGY4WEABOk40ryHY0Doz6wNFCQD1vYhYokYUNhBtT1LQ9Eccy91f6D5FKd1dhGmn7zhbp-fto8vswllnkvvkMZ8t_n9n__5i8_76vafgHJ8Wlg</recordid><startdate>20170621</startdate><enddate>20170621</enddate><creator>Pryde, D. C</creator><creator>Swain, N. A</creator><creator>Stupple, P. A</creator><creator>West, C. W</creator><creator>Marron, B</creator><creator>Markworth, C. J</creator><creator>Printzenhoff, D</creator><creator>Lin, Z</creator><creator>Cox, P. J</creator><creator>Suzuki, R</creator><creator>McMurray, S</creator><creator>Waldron, G. J</creator><creator>Payne, C. E</creator><creator>Warmus, J. S</creator><creator>Chapman, M. L</creator><scope/></search><sort><creationdate>20170621</creationdate><title>The discovery of a potent Nav1.3 inhibitor with good oral pharmacokineticsAll authors are, or were at the time of the work being undertaken, employees of Pfizer</title><author>Pryde, D. C ; Swain, N. A ; Stupple, P. A ; West, C. W ; Marron, B ; Markworth, C. J ; Printzenhoff, D ; Lin, Z ; Cox, P. J ; Suzuki, R ; McMurray, S ; Waldron, G. J ; Payne, C. E ; Warmus, J. S ; Chapman, M. L</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-rsc_primary_c7md00131b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><toplevel>online_resources</toplevel><creatorcontrib>Pryde, D. C</creatorcontrib><creatorcontrib>Swain, N. A</creatorcontrib><creatorcontrib>Stupple, P. A</creatorcontrib><creatorcontrib>West, C. W</creatorcontrib><creatorcontrib>Marron, B</creatorcontrib><creatorcontrib>Markworth, C. J</creatorcontrib><creatorcontrib>Printzenhoff, D</creatorcontrib><creatorcontrib>Lin, Z</creatorcontrib><creatorcontrib>Cox, P. J</creatorcontrib><creatorcontrib>Suzuki, R</creatorcontrib><creatorcontrib>McMurray, S</creatorcontrib><creatorcontrib>Waldron, G. J</creatorcontrib><creatorcontrib>Payne, C. E</creatorcontrib><creatorcontrib>Warmus, J. S</creatorcontrib><creatorcontrib>Chapman, M. L</creatorcontrib></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Pryde, D. C</au><au>Swain, N. A</au><au>Stupple, P. A</au><au>West, C. W</au><au>Marron, B</au><au>Markworth, C. J</au><au>Printzenhoff, D</au><au>Lin, Z</au><au>Cox, P. J</au><au>Suzuki, R</au><au>McMurray, S</au><au>Waldron, G. J</au><au>Payne, C. E</au><au>Warmus, J. S</au><au>Chapman, M. L</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The discovery of a potent Nav1.3 inhibitor with good oral pharmacokineticsAll authors are, or were at the time of the work being undertaken, employees of Pfizer</atitle><date>2017-06-21</date><risdate>2017</risdate><volume>8</volume><issue>6</issue><spage>1255</spage><epage>1267</epage><pages>1255-1267</pages><issn>2040-2503</issn><eissn>2040-2511</eissn><abstract>In this article, we describe the discovery of an aryl ether series of potent and selective Na
v
1.3 inhibitors. Based on structural analogy to a similar series of compounds we have previously shown bind to the domain IV voltage sensor region of Na
v
channels, we propose this series binds in the same location. We describe the development of this series from a published starting point, highlighting key selectivity and potency data, and several studies designed to validate Na
v
1.3 as a target for pain.
An aryl ether series of potent and selective Na
v
1.3 inhibitors is described, starting from a series of diphenymethyl amides.</abstract><doi>10.1039/c7md00131b</doi><tpages>13</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 2040-2503 |
| ispartof | |
| issn | 2040-2503 2040-2511 |
| language | eng |
| recordid | cdi_rsc_primary_c7md00131b |
| source | Royal Society Of Chemistry Journals 2008-; PubMed Central |
| title | The discovery of a potent Nav1.3 inhibitor with good oral pharmacokineticsAll authors are, or were at the time of the work being undertaken, employees of Pfizer |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-02-12T05%3A20%3A59IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-rsc&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=The%20discovery%20of%20a%20potent%20Nav1.3%20inhibitor%20with%20good%20oral%20pharmacokineticsAll%20authors%20are,%20or%20were%20at%20the%20time%20of%20the%20work%20being%20undertaken,%20employees%20of%20Pfizer&rft.au=Pryde,%20D.%20C&rft.date=2017-06-21&rft.volume=8&rft.issue=6&rft.spage=1255&rft.epage=1267&rft.pages=1255-1267&rft.issn=2040-2503&rft.eissn=2040-2511&rft_id=info:doi/10.1039/c7md00131b&rft_dat=%3Crsc%3Ec7md00131b%3C/rsc%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_id=info:pmid/&rfr_iscdi=true |