Cyanopeptide analogues: new lead structures for the design and synthesis of new thrombin inhibitors
This contribution deals with the structure-based design and syntheses of the new serine protease inhibitors RA-1001 and RA-1002, which are analogues of the blue-green algae derived cyanopeptide aeruginosin 98-B. Both compounds inhibit thrombin with Ki values of 5.6 microM and 8.7 microM, respectivel...
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| Veröffentlicht in: | Pharmazie 2002-11, Vol.57 (11), p.729-732 |
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| container_title | Pharmazie |
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| creator | RADAU, G STÜRZEBECHER, J |
| description | This contribution deals with the structure-based design and syntheses of the new serine protease inhibitors RA-1001 and RA-1002, which are analogues of the blue-green algae derived cyanopeptide aeruginosin 98-B. Both compounds inhibit thrombin with Ki values of 5.6 microM and 8.7 microM, respectively. |
| format | Article |
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Both compounds inhibit thrombin with Ki values of 5.6 microM and 8.7 microM, respectively.</description><identifier>ISSN: 0031-7144</identifier><identifier>PMID: 12611274</identifier><identifier>CODEN: PHARAT</identifier><language>eng</language><publisher>Eschborn: Govi</publisher><subject>Biological and medical sciences ; Blood. Blood coagulation. Reticuloendothelial system ; Cyanobacteria - chemistry ; Drug Design ; Fibrinolysin - chemical synthesis ; Fibrinolysin - pharmacology ; Humans ; In Vitro Techniques ; Indicators and Reagents ; Kinetics ; Magnetic Resonance Spectroscopy ; Medical sciences ; Oligopeptides - chemistry ; Oligopeptides - pharmacology ; Pharmacology. Drug treatments ; Serine Proteinase Inhibitors - chemical synthesis ; Serine Proteinase Inhibitors - pharmacology ; Spectrophotometry, Infrared ; Structure-Activity Relationship ; Thrombin - antagonists & inhibitors ; Trypsin Inhibitors - chemical synthesis ; Trypsin Inhibitors - pharmacology</subject><ispartof>Pharmazie, 2002-11, Vol.57 (11), p.729-732</ispartof><rights>2003 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=13999137$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12611274$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>RADAU, G</creatorcontrib><creatorcontrib>STÜRZEBECHER, J</creatorcontrib><title>Cyanopeptide analogues: new lead structures for the design and synthesis of new thrombin inhibitors</title><title>Pharmazie</title><addtitle>Pharmazie</addtitle><description>This contribution deals with the structure-based design and syntheses of the new serine protease inhibitors RA-1001 and RA-1002, which are analogues of the blue-green algae derived cyanopeptide aeruginosin 98-B. Both compounds inhibit thrombin with Ki values of 5.6 microM and 8.7 microM, respectively.</description><subject>Biological and medical sciences</subject><subject>Blood. Blood coagulation. Reticuloendothelial system</subject><subject>Cyanobacteria - chemistry</subject><subject>Drug Design</subject><subject>Fibrinolysin - chemical synthesis</subject><subject>Fibrinolysin - pharmacology</subject><subject>Humans</subject><subject>In Vitro Techniques</subject><subject>Indicators and Reagents</subject><subject>Kinetics</subject><subject>Magnetic Resonance Spectroscopy</subject><subject>Medical sciences</subject><subject>Oligopeptides - chemistry</subject><subject>Oligopeptides - pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Serine Proteinase Inhibitors - chemical synthesis</subject><subject>Serine Proteinase Inhibitors - pharmacology</subject><subject>Spectrophotometry, Infrared</subject><subject>Structure-Activity Relationship</subject><subject>Thrombin - antagonists & inhibitors</subject><subject>Trypsin Inhibitors - chemical synthesis</subject><subject>Trypsin Inhibitors - pharmacology</subject><issn>0031-7144</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2002</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpF0MFKxDAQBuAeFHddfQXJRW-FJukmrTdZ1BUWvOi5TJLJbqRNapIi-_YWXfE0MPPNwD9nxbKqOC0lretFcZnSR1UxwURzUSwoE5QyWS8LvTmCDyOO2Rkk4KEP-wnTPfH4RXoEQ1KOk85TxERsiCQfkBhMbu9nPU-Pfu4kl0iwPzv5EMOgnCfOH5xyOcR0VZxb6BNen-qqeH96fNtsy93r88vmYVeOjMtcKqiUBSMpXWNbK6yFNbVuAVWDtKKgpWCWiVpLo1ojBdeN1MCtRalboSRfFXe_d8cYPucQuRtc0tj34DFMqZOsWTdz7hnenOCkBjTdGN0A8dj9vWUGtycASUNvI3jt0r_jbdtSLvk38WVtPg</recordid><startdate>20021101</startdate><enddate>20021101</enddate><creator>RADAU, G</creator><creator>STÜRZEBECHER, J</creator><general>Govi</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>20021101</creationdate><title>Cyanopeptide analogues: new lead structures for the design and synthesis of new thrombin inhibitors</title><author>RADAU, G ; STÜRZEBECHER, J</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p237t-ba0bfad7115e94be46fd4c9aeb8e101ac762f264c7db9d763c87ca3ffe7c96b73</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2002</creationdate><topic>Biological and medical sciences</topic><topic>Blood. Blood coagulation. Reticuloendothelial system</topic><topic>Cyanobacteria - chemistry</topic><topic>Drug Design</topic><topic>Fibrinolysin - chemical synthesis</topic><topic>Fibrinolysin - pharmacology</topic><topic>Humans</topic><topic>In Vitro Techniques</topic><topic>Indicators and Reagents</topic><topic>Kinetics</topic><topic>Magnetic Resonance Spectroscopy</topic><topic>Medical sciences</topic><topic>Oligopeptides - chemistry</topic><topic>Oligopeptides - pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Serine Proteinase Inhibitors - chemical synthesis</topic><topic>Serine Proteinase Inhibitors - pharmacology</topic><topic>Spectrophotometry, Infrared</topic><topic>Structure-Activity Relationship</topic><topic>Thrombin - antagonists & inhibitors</topic><topic>Trypsin Inhibitors - chemical synthesis</topic><topic>Trypsin Inhibitors - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>RADAU, G</creatorcontrib><creatorcontrib>STÜRZEBECHER, J</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>MEDLINE - Academic</collection><jtitle>Pharmazie</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>RADAU, G</au><au>STÜRZEBECHER, J</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Cyanopeptide analogues: new lead structures for the design and synthesis of new thrombin inhibitors</atitle><jtitle>Pharmazie</jtitle><addtitle>Pharmazie</addtitle><date>2002-11-01</date><risdate>2002</risdate><volume>57</volume><issue>11</issue><spage>729</spage><epage>732</epage><pages>729-732</pages><issn>0031-7144</issn><coden>PHARAT</coden><abstract>This contribution deals with the structure-based design and syntheses of the new serine protease inhibitors RA-1001 and RA-1002, which are analogues of the blue-green algae derived cyanopeptide aeruginosin 98-B. Both compounds inhibit thrombin with Ki values of 5.6 microM and 8.7 microM, respectively.</abstract><cop>Eschborn</cop><pub>Govi</pub><pmid>12611274</pmid><tpages>4</tpages></addata></record> |
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| ispartof | Pharmazie, 2002-11, Vol.57 (11), p.729-732 |
| issn | 0031-7144 |
| language | eng |
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| source | MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals |
| subjects | Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Cyanobacteria - chemistry Drug Design Fibrinolysin - chemical synthesis Fibrinolysin - pharmacology Humans In Vitro Techniques Indicators and Reagents Kinetics Magnetic Resonance Spectroscopy Medical sciences Oligopeptides - chemistry Oligopeptides - pharmacology Pharmacology. Drug treatments Serine Proteinase Inhibitors - chemical synthesis Serine Proteinase Inhibitors - pharmacology Spectrophotometry, Infrared Structure-Activity Relationship Thrombin - antagonists & inhibitors Trypsin Inhibitors - chemical synthesis Trypsin Inhibitors - pharmacology |
| title | Cyanopeptide analogues: new lead structures for the design and synthesis of new thrombin inhibitors |
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