Small, non-peptide C5a receptor antagonists: Part 2
▪ Starting from 2, several highly potent C5a receptor antagonists were synthesised through α-amide substitution. Attempts to increase the polarity of these compounds through the introduction of basic centres or incorporation into weakly basic heterocycles is described.
Gespeichert in:
| Veröffentlicht in: | Bioorganic & medicinal chemistry 2008-10, Vol.18 (20), p.5605-5608 |
|---|---|
| Hauptverfasser: | , , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 5608 |
|---|---|
| container_issue | 20 |
| container_start_page | 5605 |
| container_title | Bioorganic & medicinal chemistry |
| container_volume | 18 |
| creator | Blagg, Julian Mowbray, Charles Pryde, David Salmon, Gary Fairman, David Schmid, Esther Beaumont, Kevin |
| description | ▪
Starting from
2, several highly potent C5a receptor antagonists were synthesised through α-amide substitution. Attempts to increase the polarity of these compounds through the introduction of basic centres or incorporation into weakly basic heterocycles is described. |
| doi_str_mv | 10.1016/j.bmcl.2008.08.101 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_19333766</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0960894X08010366</els_id><sourcerecordid>19333766</sourcerecordid><originalsourceid>FETCH-LOGICAL-c415t-c8d1cb66c156474b8226f8d49a7b2da2133254dc8c34c04c5d95389b1c0995183</originalsourceid><addsrcrecordid>eNp9kEtLAzEQx4Motj6-gAfZi57cNa9NE_EixRcUFFTwFrKTrKTsoyZbwW9vlha9CQPDDL_5M_wQOiG4IJiIy2VRtdAUFGNZpEq7HTQlXPCccVzuoilWAudS8fcJOohxiTHhmPN9NCFSYs6EmiL20pqmuci6vstXbjV467J5abLgIE19yEw3mI--83GIV9mzCUNGj9BebZrojrf9EL3d3b7OH_LF0_3j_GaRAyflkIO0BCohgJSCz3glKRW1tFyZWUWtoYQxWnILEhgHzKG0qmRSVQSwUiWR7BCdb3JXof9cuzjo1kdwTWM616-jJooxNhMigXQDQuhjDK7Wq-BbE741wXpUpZd6VKVHVTpV2qWj0236umqd_TvZuknA2RYwEUxTB9OBj78cxTMlCR2DrjecSy6-vAs6gncdOOuTxUHb3v_3xw-Z4oRl</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>19333766</pqid></control><display><type>article</type><title>Small, non-peptide C5a receptor antagonists: Part 2</title><source>MEDLINE</source><source>ScienceDirect Journals (5 years ago - present)</source><creator>Blagg, Julian ; Mowbray, Charles ; Pryde, David ; Salmon, Gary ; Fairman, David ; Schmid, Esther ; Beaumont, Kevin</creator><creatorcontrib>Blagg, Julian ; Mowbray, Charles ; Pryde, David ; Salmon, Gary ; Fairman, David ; Schmid, Esther ; Beaumont, Kevin</creatorcontrib><description>▪
Starting from
2, several highly potent C5a receptor antagonists were synthesised through α-amide substitution. Attempts to increase the polarity of these compounds through the introduction of basic centres or incorporation into weakly basic heterocycles is described.</description><identifier>ISSN: 0960-894X</identifier><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3405</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/j.bmcl.2008.08.101</identifier><identifier>PMID: 18804369</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Administration, Oral ; Amides - chemistry ; Antagonists ; Binding Sites ; Biological and medical sciences ; Bones, joints and connective tissue. Antiinflammatory agents ; C5a Receptor ; Chemistry, Pharmaceutical - methods ; Complement ; Complement C5a - antagonists & inhibitors ; Complement C5a - chemistry ; Drug Design ; Humans ; Hydrolysis ; Inflammation ; Inhibitory Concentration 50 ; Medical sciences ; Models, Chemical ; Molecular Structure ; Peptides - chemistry ; Pharmacology. Drug treatments ; Piperidines - chemistry ; Protein Binding</subject><ispartof>Bioorganic & medicinal chemistry, 2008-10, Vol.18 (20), p.5605-5608</ispartof><rights>2008 Elsevier Ltd</rights><rights>2009 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c415t-c8d1cb66c156474b8226f8d49a7b2da2133254dc8c34c04c5d95389b1c0995183</citedby><cites>FETCH-LOGICAL-c415t-c8d1cb66c156474b8226f8d49a7b2da2133254dc8c34c04c5d95389b1c0995183</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X08010366$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65534</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=20798121$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/18804369$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Blagg, Julian</creatorcontrib><creatorcontrib>Mowbray, Charles</creatorcontrib><creatorcontrib>Pryde, David</creatorcontrib><creatorcontrib>Salmon, Gary</creatorcontrib><creatorcontrib>Fairman, David</creatorcontrib><creatorcontrib>Schmid, Esther</creatorcontrib><creatorcontrib>Beaumont, Kevin</creatorcontrib><title>Small, non-peptide C5a receptor antagonists: Part 2</title><title>Bioorganic & medicinal chemistry</title><addtitle>Bioorg Med Chem Lett</addtitle><description>▪
Starting from
2, several highly potent C5a receptor antagonists were synthesised through α-amide substitution. Attempts to increase the polarity of these compounds through the introduction of basic centres or incorporation into weakly basic heterocycles is described.</description><subject>Administration, Oral</subject><subject>Amides - chemistry</subject><subject>Antagonists</subject><subject>Binding Sites</subject><subject>Biological and medical sciences</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>C5a Receptor</subject><subject>Chemistry, Pharmaceutical - methods</subject><subject>Complement</subject><subject>Complement C5a - antagonists & inhibitors</subject><subject>Complement C5a - chemistry</subject><subject>Drug Design</subject><subject>Humans</subject><subject>Hydrolysis</subject><subject>Inflammation</subject><subject>Inhibitory Concentration 50</subject><subject>Medical sciences</subject><subject>Models, Chemical</subject><subject>Molecular Structure</subject><subject>Peptides - chemistry</subject><subject>Pharmacology. Drug treatments</subject><subject>Piperidines - chemistry</subject><subject>Protein Binding</subject><issn>0960-894X</issn><issn>0968-0896</issn><issn>1464-3405</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2008</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kEtLAzEQx4Motj6-gAfZi57cNa9NE_EixRcUFFTwFrKTrKTsoyZbwW9vlha9CQPDDL_5M_wQOiG4IJiIy2VRtdAUFGNZpEq7HTQlXPCccVzuoilWAudS8fcJOohxiTHhmPN9NCFSYs6EmiL20pqmuci6vstXbjV467J5abLgIE19yEw3mI--83GIV9mzCUNGj9BebZrojrf9EL3d3b7OH_LF0_3j_GaRAyflkIO0BCohgJSCz3glKRW1tFyZWUWtoYQxWnILEhgHzKG0qmRSVQSwUiWR7BCdb3JXof9cuzjo1kdwTWM616-jJooxNhMigXQDQuhjDK7Wq-BbE741wXpUpZd6VKVHVTpV2qWj0236umqd_TvZuknA2RYwEUxTB9OBj78cxTMlCR2DrjecSy6-vAs6gncdOOuTxUHb3v_3xw-Z4oRl</recordid><startdate>20081015</startdate><enddate>20081015</enddate><creator>Blagg, Julian</creator><creator>Mowbray, Charles</creator><creator>Pryde, David</creator><creator>Salmon, Gary</creator><creator>Fairman, David</creator><creator>Schmid, Esther</creator><creator>Beaumont, Kevin</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></search><sort><creationdate>20081015</creationdate><title>Small, non-peptide C5a receptor antagonists: Part 2</title><author>Blagg, Julian ; Mowbray, Charles ; Pryde, David ; Salmon, Gary ; Fairman, David ; Schmid, Esther ; Beaumont, Kevin</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c415t-c8d1cb66c156474b8226f8d49a7b2da2133254dc8c34c04c5d95389b1c0995183</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2008</creationdate><topic>Administration, Oral</topic><topic>Amides - chemistry</topic><topic>Antagonists</topic><topic>Binding Sites</topic><topic>Biological and medical sciences</topic><topic>Bones, joints and connective tissue. Antiinflammatory agents</topic><topic>C5a Receptor</topic><topic>Chemistry, Pharmaceutical - methods</topic><topic>Complement</topic><topic>Complement C5a - antagonists & inhibitors</topic><topic>Complement C5a - chemistry</topic><topic>Drug Design</topic><topic>Humans</topic><topic>Hydrolysis</topic><topic>Inflammation</topic><topic>Inhibitory Concentration 50</topic><topic>Medical sciences</topic><topic>Models, Chemical</topic><topic>Molecular Structure</topic><topic>Peptides - chemistry</topic><topic>Pharmacology. Drug treatments</topic><topic>Piperidines - chemistry</topic><topic>Protein Binding</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Blagg, Julian</creatorcontrib><creatorcontrib>Mowbray, Charles</creatorcontrib><creatorcontrib>Pryde, David</creatorcontrib><creatorcontrib>Salmon, Gary</creatorcontrib><creatorcontrib>Fairman, David</creatorcontrib><creatorcontrib>Schmid, Esther</creatorcontrib><creatorcontrib>Beaumont, Kevin</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><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Blagg, Julian</au><au>Mowbray, Charles</au><au>Pryde, David</au><au>Salmon, Gary</au><au>Fairman, David</au><au>Schmid, Esther</au><au>Beaumont, Kevin</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Small, non-peptide C5a receptor antagonists: Part 2</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2008-10-15</date><risdate>2008</risdate><volume>18</volume><issue>20</issue><spage>5605</spage><epage>5608</epage><pages>5605-5608</pages><issn>0960-894X</issn><issn>0968-0896</issn><eissn>1464-3405</eissn><eissn>1464-3391</eissn><abstract>▪
Starting from
2, several highly potent C5a receptor antagonists were synthesised through α-amide substitution. Attempts to increase the polarity of these compounds through the introduction of basic centres or incorporation into weakly basic heterocycles is described.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>18804369</pmid><doi>10.1016/j.bmcl.2008.08.101</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry, 2008-10, Vol.18 (20), p.5605-5608 |
| issn | 0960-894X 0968-0896 1464-3405 1464-3391 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_19333766 |
| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | Administration, Oral Amides - chemistry Antagonists Binding Sites Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents C5a Receptor Chemistry, Pharmaceutical - methods Complement Complement C5a - antagonists & inhibitors Complement C5a - chemistry Drug Design Humans Hydrolysis Inflammation Inhibitory Concentration 50 Medical sciences Models, Chemical Molecular Structure Peptides - chemistry Pharmacology. Drug treatments Piperidines - chemistry Protein Binding |
| title | Small, non-peptide C5a receptor antagonists: Part 2 |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-02-20T18%3A05%3A33IST&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=Small,%20non-peptide%20C5a%20receptor%20antagonists:%20Part%202&rft.jtitle=Bioorganic%20&%20medicinal%20chemistry&rft.au=Blagg,%20Julian&rft.date=2008-10-15&rft.volume=18&rft.issue=20&rft.spage=5605&rft.epage=5608&rft.pages=5605-5608&rft.issn=0960-894X&rft.eissn=1464-3405&rft_id=info:doi/10.1016/j.bmcl.2008.08.101&rft_dat=%3Cproquest_cross%3E19333766%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=19333766&rft_id=info:pmid/18804369&rft_els_id=S0960894X08010366&rfr_iscdi=true |