Synthesis of novel tetrahydroisoquinoline bronchodilators
The discovery and synthesis of bronchodilator 71 using a functional tissue assay is described. The synthesis and bronchorelaxing effects of a series of novel tetrahydroisoquinoline amides are described. The compounds were evaluated for their ability to relax LTD4 contracted isolated human small airw...
Gespeichert in:
| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2010-09, Vol.20 (17), p.4999-5003 |
|---|---|
| Hauptverfasser: | , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 5003 |
|---|---|
| container_issue | 17 |
| container_start_page | 4999 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 20 |
| creator | Dalence-Guzmán, Maria F. Toftered, Jörgen Oltner, Viveca Thornqvist Wensbo, David Johansson, Martin H. |
| description | The discovery and synthesis of bronchodilator
71 using a functional tissue assay is described.
The synthesis and bronchorelaxing effects of a series of novel tetrahydroisoquinoline amides are described. The compounds were evaluated for their ability to relax LTD4 contracted isolated human small airways ex-vivo. Several compounds demonstrated highly efficacious bronchorelaxing properties. Cinnamide 71 was selected for further studies and constitutes a promising candidate as a novel bronchorelaxing agent for the treatment of pulmonary disorders. |
| doi_str_mv | 10.1016/j.bmcl.2010.07.057 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_748974692</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0960894X10010139</els_id><sourcerecordid>748974692</sourcerecordid><originalsourceid>FETCH-LOGICAL-c385t-f2a91631d17c6d90855f7bdbbb413b12ced7a1aca12b5cd7bb91a24be774b5de3</originalsourceid><addsrcrecordid>eNp9kMtKAzEUhoMotl5ewIV0I66mJplcJuBGxBsILlRwF3I5Q1Omk5pMhb69Ka26c3Xg8P0_53wInRE8JZiIq_nULlw3pbgssJxiLvfQmDDBqpphvo_GWAlcNYp9jNBRznOMCcOMHaIRxUI2quZjpF7X_TCDHPIktpM-fkE3GWBIZrb2KYYcP1ehj13oYWJT7N0s-tCZIaZ8gg5a02U43c1j9H5_93b7WD2_PDzd3jxXrm74ULXUKCJq4ol0wivccN5K6621jNSWUAdeGmKcIdRy56W1ihjKLEjJLPdQH6PLbe8ylWMgD3oRsoOuMz3EVdaSNUoyoWgh6ZZ0KeacoNXLFBYmrTXBemNMz_XGmN4Y01jqYqyEznf1K7sA_xv5UVSAix1gsjNdm0zvQv7jatJQwUXhrrccFBlfAZLOLkBf_gsJ3KB9DP_d8Q0ioYs9</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>748974692</pqid></control><display><type>article</type><title>Synthesis of novel tetrahydroisoquinoline bronchodilators</title><source>MEDLINE</source><source>Access via ScienceDirect (Elsevier)</source><creator>Dalence-Guzmán, Maria F. ; Toftered, Jörgen ; Oltner, Viveca Thornqvist ; Wensbo, David ; Johansson, Martin H.</creator><creatorcontrib>Dalence-Guzmán, Maria F. ; Toftered, Jörgen ; Oltner, Viveca Thornqvist ; Wensbo, David ; Johansson, Martin H.</creatorcontrib><description>The discovery and synthesis of bronchodilator
71 using a functional tissue assay is described.
The synthesis and bronchorelaxing effects of a series of novel tetrahydroisoquinoline amides are described. The compounds were evaluated for their ability to relax LTD4 contracted isolated human small airways ex-vivo. Several compounds demonstrated highly efficacious bronchorelaxing properties. Cinnamide 71 was selected for further studies and constitutes a promising candidate as a novel bronchorelaxing agent for the treatment of pulmonary disorders.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2010.07.057</identifier><identifier>PMID: 20678935</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Asthma ; Biological and medical sciences ; Bones, joints and connective tissue. Antiinflammatory agents ; Bronchi - drug effects ; Bronchodilator ; Bronchodilator Agents - chemical synthesis ; Bronchodilator Agents - chemistry ; Bronchodilator Agents - pharmacology ; COPD ; Humans ; In Vitro Techniques ; Isoquinolines - chemical synthesis ; Isoquinolines - chemistry ; Isoquinolines - pharmacology ; Medical sciences ; Palladium catalyzed cross-coupling ; Pharmacology. Drug treatments ; Respiratory system ; Structure-Activity Relationship ; Tetrahydroisoquinoline</subject><ispartof>Bioorganic & medicinal chemistry letters, 2010-09, Vol.20 (17), p.4999-5003</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-c385t-f2a91631d17c6d90855f7bdbbb413b12ced7a1aca12b5cd7bb91a24be774b5de3</citedby><cites>FETCH-LOGICAL-c385t-f2a91631d17c6d90855f7bdbbb413b12ced7a1aca12b5cd7bb91a24be774b5de3</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.2010.07.057$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=23182656$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/20678935$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Dalence-Guzmán, Maria F.</creatorcontrib><creatorcontrib>Toftered, Jörgen</creatorcontrib><creatorcontrib>Oltner, Viveca Thornqvist</creatorcontrib><creatorcontrib>Wensbo, David</creatorcontrib><creatorcontrib>Johansson, Martin H.</creatorcontrib><title>Synthesis of novel tetrahydroisoquinoline bronchodilators</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>The discovery and synthesis of bronchodilator
71 using a functional tissue assay is described.
The synthesis and bronchorelaxing effects of a series of novel tetrahydroisoquinoline amides are described. The compounds were evaluated for their ability to relax LTD4 contracted isolated human small airways ex-vivo. Several compounds demonstrated highly efficacious bronchorelaxing properties. Cinnamide 71 was selected for further studies and constitutes a promising candidate as a novel bronchorelaxing agent for the treatment of pulmonary disorders.</description><subject>Asthma</subject><subject>Biological and medical sciences</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>Bronchi - drug effects</subject><subject>Bronchodilator</subject><subject>Bronchodilator Agents - chemical synthesis</subject><subject>Bronchodilator Agents - chemistry</subject><subject>Bronchodilator Agents - pharmacology</subject><subject>COPD</subject><subject>Humans</subject><subject>In Vitro Techniques</subject><subject>Isoquinolines - chemical synthesis</subject><subject>Isoquinolines - chemistry</subject><subject>Isoquinolines - pharmacology</subject><subject>Medical sciences</subject><subject>Palladium catalyzed cross-coupling</subject><subject>Pharmacology. Drug treatments</subject><subject>Respiratory system</subject><subject>Structure-Activity Relationship</subject><subject>Tetrahydroisoquinoline</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMtKAzEUhoMotl5ewIV0I66mJplcJuBGxBsILlRwF3I5Q1Omk5pMhb69Ka26c3Xg8P0_53wInRE8JZiIq_nULlw3pbgssJxiLvfQmDDBqpphvo_GWAlcNYp9jNBRznOMCcOMHaIRxUI2quZjpF7X_TCDHPIktpM-fkE3GWBIZrb2KYYcP1ehj13oYWJT7N0s-tCZIaZ8gg5a02U43c1j9H5_93b7WD2_PDzd3jxXrm74ULXUKCJq4ol0wivccN5K6621jNSWUAdeGmKcIdRy56W1ihjKLEjJLPdQH6PLbe8ylWMgD3oRsoOuMz3EVdaSNUoyoWgh6ZZ0KeacoNXLFBYmrTXBemNMz_XGmN4Y01jqYqyEznf1K7sA_xv5UVSAix1gsjNdm0zvQv7jatJQwUXhrrccFBlfAZLOLkBf_gsJ3KB9DP_d8Q0ioYs9</recordid><startdate>20100901</startdate><enddate>20100901</enddate><creator>Dalence-Guzmán, Maria F.</creator><creator>Toftered, Jörgen</creator><creator>Oltner, Viveca Thornqvist</creator><creator>Wensbo, David</creator><creator>Johansson, Martin H.</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>7X8</scope></search><sort><creationdate>20100901</creationdate><title>Synthesis of novel tetrahydroisoquinoline bronchodilators</title><author>Dalence-Guzmán, Maria F. ; Toftered, Jörgen ; Oltner, Viveca Thornqvist ; Wensbo, David ; Johansson, Martin H.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c385t-f2a91631d17c6d90855f7bdbbb413b12ced7a1aca12b5cd7bb91a24be774b5de3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>Asthma</topic><topic>Biological and medical sciences</topic><topic>Bones, joints and connective tissue. Antiinflammatory agents</topic><topic>Bronchi - drug effects</topic><topic>Bronchodilator</topic><topic>Bronchodilator Agents - chemical synthesis</topic><topic>Bronchodilator Agents - chemistry</topic><topic>Bronchodilator Agents - pharmacology</topic><topic>COPD</topic><topic>Humans</topic><topic>In Vitro Techniques</topic><topic>Isoquinolines - chemical synthesis</topic><topic>Isoquinolines - chemistry</topic><topic>Isoquinolines - pharmacology</topic><topic>Medical sciences</topic><topic>Palladium catalyzed cross-coupling</topic><topic>Pharmacology. Drug treatments</topic><topic>Respiratory system</topic><topic>Structure-Activity Relationship</topic><topic>Tetrahydroisoquinoline</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Dalence-Guzmán, Maria F.</creatorcontrib><creatorcontrib>Toftered, Jörgen</creatorcontrib><creatorcontrib>Oltner, Viveca Thornqvist</creatorcontrib><creatorcontrib>Wensbo, David</creatorcontrib><creatorcontrib>Johansson, Martin H.</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>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Dalence-Guzmán, Maria F.</au><au>Toftered, Jörgen</au><au>Oltner, Viveca Thornqvist</au><au>Wensbo, David</au><au>Johansson, Martin H.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis of novel tetrahydroisoquinoline bronchodilators</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2010-09-01</date><risdate>2010</risdate><volume>20</volume><issue>17</issue><spage>4999</spage><epage>5003</epage><pages>4999-5003</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>The discovery and synthesis of bronchodilator
71 using a functional tissue assay is described.
The synthesis and bronchorelaxing effects of a series of novel tetrahydroisoquinoline amides are described. The compounds were evaluated for their ability to relax LTD4 contracted isolated human small airways ex-vivo. Several compounds demonstrated highly efficacious bronchorelaxing properties. Cinnamide 71 was selected for further studies and constitutes a promising candidate as a novel bronchorelaxing agent for the treatment of pulmonary disorders.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>20678935</pmid><doi>10.1016/j.bmcl.2010.07.057</doi><tpages>5</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2010-09, Vol.20 (17), p.4999-5003 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_748974692 |
| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Asthma Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Bronchi - drug effects Bronchodilator Bronchodilator Agents - chemical synthesis Bronchodilator Agents - chemistry Bronchodilator Agents - pharmacology COPD Humans In Vitro Techniques Isoquinolines - chemical synthesis Isoquinolines - chemistry Isoquinolines - pharmacology Medical sciences Palladium catalyzed cross-coupling Pharmacology. Drug treatments Respiratory system Structure-Activity Relationship Tetrahydroisoquinoline |
| title | Synthesis of novel tetrahydroisoquinoline bronchodilators |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-29T16%3A37%3A32IST&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=Synthesis%20of%20novel%20tetrahydroisoquinoline%20bronchodilators&rft.jtitle=Bioorganic%20&%20medicinal%20chemistry%20letters&rft.au=Dalence-Guzm%C3%A1n,%20Maria%20F.&rft.date=2010-09-01&rft.volume=20&rft.issue=17&rft.spage=4999&rft.epage=5003&rft.pages=4999-5003&rft.issn=0960-894X&rft.eissn=1464-3405&rft_id=info:doi/10.1016/j.bmcl.2010.07.057&rft_dat=%3Cproquest_cross%3E748974692%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=748974692&rft_id=info:pmid/20678935&rft_els_id=S0960894X10010139&rfr_iscdi=true |